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GDC-0879
GDC-0879, a highly selective, potent, and orally bioavailable RAF small-molecule inhibitor. In GDC-0879-treated mice, both cell line- and patient-derived BRAF(V600E) tumors exhibited stronger and more sustained pharmacodynamic inhibition (>90% for 8 hours) and improved survival compared with mutant KRAS-expressing tumors. Despite the involvement of activated RAF signaling in RAS-induced tumorigenesis, decreased time to progression was observed for some KRAS-mutant tumors following GDC-0879 administration. Moreover, striking differences were noted for RAF and MEK inhibition across a panel of 130 tumor cell lines. Whereas GDC-0879-mediated efficacy was associated strictly with BRAF(V600E) status, MEK inhibition also attenuated proliferation and tumor growth of cell lines expressing wild-type BRAF (81% KRAS mutant, 38% KRAS wild type). The responsiveness of BRAF(V600E) melanoma cells to GDC-0879 could be dramatically altered by pharmacologic and genetic modulation of phosphatidylinositol 3-kinase pathway activity. These data suggest that GDC-0879-induced signaling changes are dependent on the point of oncogenic activation within the RAS network. Taken together, these studies increase our understanding of the molecular determinants for antitumor efficacy resulting from RAF pathway inhibition and have implications for therapeutic intervention in the clinic. Synonyms: GDC0879; GDC-0879; GDC 0879. CAS No. 905281-76-7. Molecular formula: C19H18N4O2. Mole weight: 334.37182.
GDC-0917
CUDC-427, also known as, GDC-0917, is an orally available, monovalent mimetic of second mitochondrial-derived activator of caspases (Smac/DIABLO) and inhibitor of IAPs (Inhibitor of Apoptosis Proteins) with potential antineoplastic activity. Smac mimetic CUDC-427 binds to the Smac binding groove on IAPs, including the direct caspase inhibitor X chromosome-linked IAP (XIAP) and the cellular IAPs 1 and 2. This inhibits the activities of these IAPs and promotes the induction of apoptosis through apoptotic signaling pathways. IAPs are overexpressed by many cancer cell types and suppress apoptosis by binding to and inhibiting active caspases-3, -7 and -9 via their baculoviral lAP repeat (BIR) domains. Synonyms: GDC-0917; GDC0917; GDC 0917; CUDC-427; CUDC427; CUDC-427. Grades: 0.98. CAS No. 1446182-94-0. Molecular formula: C29H36N6O4S. Mole weight: 564.705.
GDC-0927
GDC-0927 (SRN-927) is a selective oral estrogen receptor degrader (SERD) in a phase I clinical trial for the treatment of postmenopausal women with locally advanced or metastatic estrogen receptor positive breast cancer. Study shows well tolerability and clinical effect. Uses: The potential therapy of breast cancer caused by estrogen disorder. Synonyms: SRN-927; SRN 927; SRN927; GDC-0927; GDC 0927; GDC0927. CAS No. 1642297-01-5. Molecular formula: C28H28FNO4. Mole weight: 461.52.
GDC-0941 dimethanesulfonate
GDC-0941 dimethanesulfonate is a potent inhibitor of PI3Kα/δ with modest selectivity against p110β and p110&gamma. It is a novel selective class I phosphatidylinositol-3-kinase (PI3K) inhibitor. It is designed to bind the ATP-binding pocket of PI3K and to prevent formation of phosphatidylinositol-3, 4, 5-triphosphate (PIP3), a second messenger that transmits PI3K downstream signals. It causes growth inhibition in a variety of cancer cell lines, including A2780, MDA-MB-361, PC3, and U87MG. It also inhibits the growth of trastuzumab-sensitive and -resistant HER2-amplied cancer cells which harbor p110( mutations or PTEN loss. It also reduces tumor volume in different xenograft models. Synonyms: GDC-0941 dimethanesulfonate; GDC 0941 dimethanesulfonate; GDC0941 dimethanesulfonate; Pictilisib dimethanesulfonate; GDC-0941 (2 MeSO3H salt). Grades: >98%. CAS No. 957054-33-0. Molecular formula: C25H35N7O9S4. Mole weight: 705.85.
Gedatolisib (PF-05212384, PKI-587)
Gedatolisib (PF-05212384, PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ and mTOR with IC50 of 0.4 nM, 5.4 nM and 1.6 nM, respectively. Phase 2. Synonyms: PKI587; PKI-587; PKI 587; PF05212384; PF-05212384; PF 05212384; PF5212384; PF-5212384; PF 5212384; Gedatolisib. Grades: >98%. CAS No. 1197160-78-3. Molecular formula: C32H41N9O4. Mole weight: 615.73.
Gefitinib hydrochloride
Gefitinib Hcl(ZD-1839 Hcl) is an EGFR inhibitor, which interrupts signaling through the epidermal growth factor receptor (EGFR) in target cells. Synonyms: Iressa hydrochloride; ZD 1839 hydrochloride; ZD-1839 hydrochloride; ZD1839 hydrochloride. Grades: >98%. CAS No. 184475-55-6. Molecular formula: C22H25Cl2FN4O3. Mole weight: 483.36.
Gemfibrozil
Gemfibrozil is the generic name for an oral drug used to lower lipid levels. It belongs to a group of drugs known as fibrates. It is most commonly sold as the brand name, Lopid. Other brand names include Jezil and Gen-Fibro. Synonyms: CI-719; CI 719;CI719. Grades: >98%. CAS No. 25812-30-0. Molecular formula: C15H22O3. Mole weight: 250.33.
Gemigliptin
Gemigliptin is a potent dipeptidyl peptidase-4 (DPP-4) inhibitor with the potential use in diabetes treatment. Synonyms: 1-[(2S)-2-amino-4-[2,4-bis(trifluoromethyl)-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-7-yl]-4-oxobutyl]-5,5-difluoropiperidin-2-one. CAS No. 911637-19-9. Molecular formula: C18H19F8N5O2. Mole weight: 489.37.
Gemilukast
This active molecular is an potent dual Leukotriene CysLT1 and CysLT2 Receptor antagonist originated by Ono Pharmaceutical. IC50 values is 1.7nM against human CysLT1 and 25 nM against human CysLT2. Gemilukast reduced LTC4-induced bronchoconstriction in asthmatic animal models dose-dependently. In addition, it can also reduceantigen-induced constriction of isolated human bronchi. In 2015, Phase-II clinical trials in Asthma in Japan and USA was on-going. Uses: Asthma. Synonyms: ONO6950; ONO 6950; ONO-6950;4,4'-(4-fluoro-7-((4-(4-(3-fluoro-2-methylphenyl)butoxy)phenyl)ethynyl)-2-methyl-1H-indole-1,3-diyl)dibutyric acid;1232861-64-1 (disodium salt); 1232873-69-6 (8 hydrate and disodium salt). Grades: 98%. CAS No. 1232861-58-3. Molecular formula: C36H37F2NO5. Mole weight: 601.69.
Gemopatrilat
Gemopatrilat, an azepan derivative, has been found to be an angiotensin receptor as well as vasopeptidase inhibitor that was once studied against hypertension and heart failure. Uses: Vasopeptidase inhibitors. Synonyms: Gemopatrilat; BMS 189921; BMS-189921; BMS189921; SCHEMBL1973289; {(6S)-2,2-dimethyl-7-oxo-6-[(3-phenyl-2-sulfanylpropanoyl)amino]azepan-1-yl}acetic acid; 2-[2,2-dimethyl-7-oxo-6-[(3-phenyl-2-sulfanylpropanoyl)amino]azepan-1-yl]acetic acid. Grades: 98%. CAS No. 160135-92-2. Molecular formula: C19H26N2O4S. Mole weight: 378.49.
GENZ-644282
Genz-644282 is a non-camptothecin inhibitor of topoisomerase I with potential antineoplastic activity. Topoisomerase I inhibitor Genz-644282 binds to and inhibits the enzyme topoisomerase I, which may result in the inhibition of repair of single-strand DNA breaks, DNA replication, and tumor cell growth in susceptible tumor cell populations. Synonyms: GENZ-644282; GENZ644282; GENZ 644282. CAS No. 529488-28-6. Molecular formula: C24H22F3N3O7. Mole weight: 521.44.
Geranylgeranylacetone
Geranylgeranylacetone is commonly utilized to protect the gastric mucosa in peptic ulcer disease can induce expression of HSP70, HSPB8, and HSPB1. Uses: An anti-ulcerative. Synonyms: Teprenone; 6,10,14,18-Tetramethyl-5,9,13,17-nonadecatetraen-2-one. Grades: ≥95%. CAS No. 6809-52-5. Molecular formula: C23H38O. Mole weight: 330.55.
GI 530159
GI 530159 is a TREK1 and TREK2 channel activator exhibiting selectivity for TREK1/2 over TRAAK, TASK3 and a range of other potassium channels. Synonyms: 4,4'-[[2,2,2-Trifluoro-1-(trifluoromethyl)ethylidene]bis(4,1-phenyleneoxy)]bis[benzenamine]; 4,4'-(Hexafluoroisopropylidene)bis(p-phenyleneoxy)dianiline. Grades: ≥ 99 % by HPLC. CAS No. 69563-88-8. Molecular formula: C27H20F6N2O2. Mole weight: 518.45.
Giredestrant
Giredestrant is an orally active and selective ER antagonist with anti-tumor activity. Synonyms: GDC-9545. Grades: ≥98% by HPLC. CAS No. 1953133-47-5. Molecular formula: C27H31F5N4O. Mole weight: 522.6.
Giripladib
Giripladib is a Phospholipase A2 inhibitor. Treatment with Giripladib attenuated radiation induced increases of phospho-ERK and phospho-Akt in endothelial cells. Giripladib in combination with irradiation significantly reduced migration and proliferation in endothelial cells and induced cell death and attenuated invasion by tumor cells. Uses: Antitumor. Synonyms: PLA-695; PLA 695; PLA695; Giripladib; 4-[3-[5-Chloro-1- (diphenylmethyl) -2-[2-[[[[2- (trifluoromethyl) phenyl]methyl]sulfonyl]amino]ethyl]-1H-indol-3-yl]propyl]benzoic Acid; 4- (3-[5-Chloro-1- (diphenylmethyl) -2-[2- ( ( (2- (trifluoromethyl) benzyl) sulfonyl) amino) ethyl]-1H-indole-3-yl]propyl) benzoic Acid; PLA 695. Grades: 98%. CAS No. 865200-20-0. Molecular formula: C41H36ClF3N2O4S. Mole weight: 745.25.
Gisadenafil besylate
Gisadenafil besylate is a potent PDE5 inhibitor (IC50 = 1.23 nM) with >100-fold selectivity for PDE5 over PDE6. Gisadenafil besylate inhibits the breakdown of cyclic phosphodiester secondary messenger molecules. Synonyms: UK 369003; UK369003; UK-369003; 5-[2-Ethoxy-5-[(4-ethyl-1-piperazinyl)sulfonyl]-3-pyridinyl]-3-ethyl-2,6-dihydro-2-(2-methoxyethyl)-7H-pyrazolo[4,3-d]pyrimidin-7-one benzenesulfonate. Grades: ≥99% by HPLC. CAS No. 334827-98-4. Molecular formula: C23H33N7O5S.C6H6O3S. Mole weight: 677.79.
Givinostat
Givinostat (INN) or gavinostat, aslo known as ITF2357, is a histone deacetylase inhibitor with potential anti-inflammatory, anti-angiogenic, and antineoplastic activities. It is a hydroxamate used in the form of its hydrochloride. Givinostat is in numerous phase II clinical trials (including for relapsed leukemias and myelomas), and has been granted orphan drug designation in the European Union for the treatment of systemic juvenile idiopathic arthritis and polycythaemia vera. ITF2357 was discovered at Italfarmaco of Milan, Italy. It was patented in 1997 and first described in the scientific literature in 2005. Synonyms: Givinostat; gavinostat; ITF-2357; ITF 2357; ITF2357. CAS No. 497833-27-9. Molecular formula: C24H27N3O4. Mole weight: 421.497.
Givinostat hydrochloride
Givinostat hydrochloride is the hydrochloride salt form of Givinostat. Givinostat, also called as GVS or ITF2357, a potent HDAC inhibitor for Maize HD2 (IC50= 10 nM), HD1-B (IC50= 7.5 nM nM) and HD1-A (IC50= 16 nM), has antiproliferative and proapoptotic. Uses: Histone deacetylase inhibitors. Synonyms: (6-((diethylamino)methyl)naphthalen-2-yl)methyl (4-(hydroxycarbamoyl)phenyl)carbamate hydrochloride; ITF2357; ITF-2357; ITF 2357; ITF2357 HCl; ITF2357 hydrochloride; Givinostat HCl gavinostat. CAS No. 199657-29-9. Molecular formula: C24H28ClN3O4. Mole weight: 457.95.
Givinostat hydrochloride monohydrate
Givinostat, also known as ITF2357, is an orally active HDAC inhibitor (IC50= 198 and 157 nM for HDAC1 and HDAC3, respectively), with potential anti-inflammatory, anti-angiogenic, and antineoplastic properties. Uses: Histone deacetylase inhibitors. Synonyms: [6-(diethylaminomethyl)naphthalen-2-yl]methyl N-[4-(hydroxycarbamoyl)phenyl]carbamate; hydrate; hydrochloride; givinostat hydrochloride; ITF 2357; ITF2357; ITF-2357; ITF2357 HCl; ITF2357 hydrochloride. CAS No. 732302-99-7. Molecular formula: C24H27N3O4.HCl.H2O. Mole weight: 475.97.
GK187
GK187 is a highly potent and selective inhibitor of Group VIA (GVIA) calcium-independent phospholipase A2 (iPLA2). Synonyms: 1,1,1,2,2-pentafluoro-7-(4-methoxyphenyl)-3-heptanone. Grades: ≥95%. CAS No. 1071001-50-7. Molecular formula: C14H15F5O2. Mole weight: 310.26.
GKA 50
GKA 50 is a potent glucokinase activator (EC50 = 33 nM). It causes a decrease in plasma glucose levels in diabetic rats and an increase of insulin release from mouse islets of Langerhans. GKA 50 was shown to promote proliferation and prevent apoptosis in rat pancreatic insulinoma-1 beta cell. Synonyms: GKA 50; GKA50; GKA-50; 6-[[3-[(1S)-2-Methoxy-1-methylethoxy]-5-[(1S)-1-methyl-2-phenylethoxy]benzoyl]amino-3-pyridinecarboxylic acid. Grades: ≥98% by HPLC. CAS No. 851884-87-2. Molecular formula: C26H28N2O6. Mole weight: 464.51.
Glesatinib
Glasatinib (MGCD265) is a dual MET/SMO inhibitor. Glesatinib is a small molecule, multi-target tyrosine kinase inhibitor with potential anti-tumor activity, which can antagonize P-glycoprotein (P-gp)-mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC). Synonyms: MGCD-265; MGCD 265; MGCD265. Grades: ≥98% by HPLC. CAS No. 936694-12-1. Molecular formula: C31H27F2N5O3S2. Mole weight: 619.7.
Glesatinib hydrochloride
The hydrochloride salt form of Glesatinib, an inhibitor of tyrosine kinase, could be effectively targeting tumors that are driving to grow through MET and AXL receptor. It seems to be more common in non-small cell lung cancer and it is still under Phase I. Uses: The hydrochloride salt form of glesatinib could be effectively targeting tumors that are driving to grow through met and axl receptor. Synonyms: MGCD265 hydrochloride; MGCD-265 hydrochloride; MGCD 265 hydrochloride. Grades: 98%. CAS No. 1123838-51-6. Molecular formula: C31H27ClF2N5O3S2X. Mole weight: 655.16.
GLP-1 (7-36) amide trifluoroacetate salt
GLP-1 (7-36) amide is an important peptide hormone that displays a strong insulinotropic effect. It binds the GLP-1 receptor (pIC50 = 8.5) in the pancreas and shows various antidiabetic effects. Synonyms: Glucagon-like Peptide 1 (7-36) amide. Mole weight: 3297.6.
GLP-1 (9-36) amide
GLP-1 (9-36) amide is an N-terminal truncated metabolite of glucagon-like peptide GLP-1-(7-36) formed by dipeptidyl peptidase-IV cleavage. GLP-1 (9-36) amide functions as a human GLP-1 receptor antagonist. Synonyms: Glucagon-like peptide-1 (9-36) amide; Glucagon-like peptide-1 (9 36) amide. CAS No. 161748-29-4. Molecular formula: C140H214N36O43. Mole weight: 3089.44.
The apelin gene encodes a pre-proprotein that is processed to generate bioactive peptides consisting of 36, 17, or 13 amino acids: apelin-36 , apelin-17, and apelin-13, respectively. Synonyms: (pGlu1)Apelin-13; Pyr-Apelin-13; (Pyr1)Apelin-13; 5-oxo-L-prolyl-L-arginyl-L-prolyl-L-arginyl-L-leucyl-L-seryl-L-histidyl-L-lysylglycyl-L-prolyl-L-methionyl-L-prolyl-L-phenylalanine trifluoroacetate salt. Grades: ≥95%. Molecular formula: C69H108N22O16S·xCF3COOH. Mole weight: 1533.80.
GLP-1R agonist DMB
GLP-1R agonist DMB is a glucagon-like peptide-1 (GLP-1) receptor agonist used potentially for the treatment of type 2 diabetes. Uses: Potential treatment of type 2 diabetes. Synonyms: N-(tert-Butyl)-6,7-dichloro-3-(methylsulfonyl)quinoxalin-2-amine. Grades: 99%. CAS No. 281209-71-0. Molecular formula: C13H15Cl2N3O2S. Mole weight: 348.25.
GLP-2 (rat)
GLP-2 (rat) is an endogenous peptide that acts as an intestinal epithelium-specific growth factor. It stimulates cell proliferation and inhibits apoptosis, and also modulates intestinal glucose transport, food intake, and gastric acid secretion. Synonyms: Preproglucagon (146-178) (rat); H-His-Ala-Asp-Gly-Ser-Phe-Ser-Asp-Glu-Met-Asn-Thr-Ile-Leu-Asp-Asn-Leu-Ala-Thr-Arg-Asp-Phe-Ile-Asn-Trp-Leu-Ile-Gln-Thr-Lys-Ile-Thr-Asp-OH; Glucagon-like Peptide 2 (rat); L-histidyl-L-alanyl-L-alpha-aspartyl-glycyl-L-seryl-L-phenylalanyl-L-seryl-L-alpha-aspartyl-L-alpha-glutamyl-L-methionyl-L-asparagyl-L-threonyl-L-isoleucyl-L-leucyl-L-alpha-aspartyl-L-asparagyl-L-leucyl-L-alanyl-L-threonyl-L-arginyl-L-alpha-aspartyl-L-phenylalanyl-L-isoleucyl-L-asparagyl-L-tryptophyl-L-leucyl-L-isoleucyl-L-glutaminyl-L-threonyl-L-lysyl-L-isoleucyl-L-threonyl-L-aspartic acid. Grades: ≥95%. CAS No. 195262-56-7. Molecular formula: C166H256N44O56S. Mole weight: 3796.17.
GLP-2 (rat) trifluoroacetate salt
GLP-2 is a gut peptide hormone that is primarily produced by enteroendocrine L cells of the small and large intestine. GLP-2 is an antagonist of the GLP-2 receptor (GLP-2R; Ki = 60 pM). Synonyms: Glucagon-like Peptide 2. Grades: ≥95%. Molecular formula: C166H256N44O56S·xCF3COOH. Mole weight: 3796.14.
GLPG0492
GLPG0492, a selective androgen receptor modulator, could be effective in decreasing muscle loss. The treatment study against Duchenne muscular dystrophy of it has alreadt been discontinued. Uses: Glpg0492 is a selective androgen receptor modulator that could be effective in decreasing muscle loss. Synonyms: DT-200; DT 200; DT200; GLPG0492; SCHEMBL2021011; CHEMBL2178100; GLPG 0492; GLPG-0492; VAJGULUVTFDTAS-GOSISDBHSA-N. Grades: 98%. CAS No. 1215085-92-9. Molecular formula: C19H14F3N3O3. Mole weight: 389.33.
GLPG0492 R enantiomer
The R-enantiomer of GLPG0492 which is a selective androgen receptor modulator, could be effective in decreasing muscle loss. Uses: The r-enantiomer of glpg0492 which is a selective androgen receptor modulator that could be effective in decreasing muscle loss. Synonyms: GLPG-0492 R enantiomer; GLPG 0492 R enantiomer; GLPG0492 R enantiomer. Grades: 98%. CAS No. 1215085-93-0. Molecular formula: C19H14F3N3O3. Mole weight: 389.33.
GLPG1837
GLPG1837 is a potent, orally available potentiator of cystic fibrosis transmembrane conductance regulator (CFTR) with EC50 of 3 nM and 339 nM on F508del and G551D CFTR, respectively. Synonyms: ABBV-974; N-[3-(aminocarbonyl)-4,7-dihydro-5,5,7,7-tetramethyl-5H-thieno[2,3-c]pyran-2-yl]-1H-pyrazole-3-carboxamide. Grades: ≥98%. CAS No. 1654725-02-6. Molecular formula: C16H20N4O3S. Mole weight: 348.42.
Glucagon Receptor Antagonist I
Glucagon receptor antagonist I is a potent and competitive antagonist of the glucagon receptor (GCGR) with an IC50 value of 181 nM. Synonyms: GCGR Antagonist I; hGCGR Antagonist; N-[3-cyano-6-(1,1-dimethylpropyl)-4,5,6,7-tetrahydrobenzo[b]thien-2-yl]-2-ethyl-butanamide. Grades: ≥99%. CAS No. 438618-32-7. Molecular formula: C20H30N2OS. Mole weight: 346.5.
Glucagon receptor antagonists 1
Glucagon receptor antagonists-1 is a highly potent glucagon receptor antagonist, which is activated by glucagon and is a member of the class B G-protein coupled family of receptors. Uses: Glucagon receptor antagonist. Synonyms: glucagon receptor antagonists 1; 1-(4-(2-(Benzyloxy)-4-fluorophenyl)-2,6-diisopropyl-5-(prop-1-en-1-yl)pyridin-3-yl)ethanol; 1-[4-(4-fluoro-2-phenylmethoxyphenyl)-2,6-di(propan-2-yl)-5-[(E)-prop-1-enyl]pyridin-3-yl]ethanol. Grades: ≥95%. CAS No. 503559-84-0. Molecular formula: C29H34FNO2. Mole weight: 447.59.
glucagon receptor antagonists-2
glucagon receptor antagonists-2 is a highly potent antagonist of glucagon receptor. Synonyms: glucagon receptor antagonists 2; (6E)-3-fluoro-6-[3-[(1R)-1-hydroxyethyl]-2,6-di(propan-2-yl)-5-propyl-1H-pyridin-4-ylidene]cyclohexa-2,4-dien-1-one3-Pyridinemethanol, 4-(4-fluoro-2-hydroxyphenyl)-a-methyl-2,6-bis(1-methylethyl)-5-propyl-, (aR)-. CAS No. 202917-18-8. Molecular formula: C22H30FNO2. Mole weight: 359.48.
glucagon receptor antagonists-3
glucagon receptor antagonists-3 is a highly potent antagonist of glucagon receptor. Synonyms: glucagon receptor antagonists 3; 3-Pyridinemethanol, 4-(4-fluoro-2-hydroxyphenyl)-a-methyl-2,6-bis(1-methylethyl)-5-propyl-, (aR,4R)-rel- (9CI);(aphlaR,4R)-4-(4-Fluoro-2-hydroxyphenyl)-alpha-methyl-2,6-bis(1-methylethyl)-5-propyl-3-pyridinemethanol. CAS No. 202917-17-7. Molecular formula: C22H30FNO2. Mole weight: 359.48.
glucagon receptor antagonists-4
glucagon receptor antagonists-4 is a potent glucagon receptor antagonist with great oral bioavailability in vivo. Synonyms: PF-06291874; PF 06291874; PF06291874; PF-6291874; PF 6291874; PF6291874; glucagon receptor antagonists 4; β-Alanine, N-[4-[(1S)?-1-[3,?5-dimethyl-4-[4-(trifluoromethyl)?-1H-pyrazol-1-yl]?phenoxy]?butyl]?benzoyl]?-. CAS No. 1393124-08-7. Molecular formula: C26H28F3N3O4. Mole weight: 503.51.
Glucocorticoid receptor agonist
Glucocorticoid receptor agonist is an effective Glucocorticoid receptor agonist and probably has steroid-like anti-inflammatory properties. Uses: Glucocorticoid receptor agonist is an effective glucocorticoid receptor agonist and probably has steroid-like anti-inflammatory properties. Synonyms: 4-fluoro-2-[(4R)-5, 5, 5-trifluoro-4-hydroxy-2-methyl-4-(1H-pyrrolo[2, 3-c]pyridin-2-ylmethyl)pentan-2-yl]phenol; Glucocorticoidreceptoragonist; CHEMBL1253898; 1245526-82-2; C20H20F4N2O2; 3695AH. Grades: 95%. CAS No. 1245526-82-2. Molecular formula: C20H20F4N2O2. Mole weight: 396.38.
Glumetinib
Glumetinib (SCC244) is a potent and highly selective c-Met inhibitor with an IC50 value of 0.42 nM, which displays > 2,400-fold selectivity for c-Met over those 312 kinases evaluated. Synonyms: SCC244; 6-(1-methyl-1H-pyrazol-4-yl)-1-[[6-(1-methyl-1H-pyrazol-4-yl)imidazo[1,2-a]pyridin-3-yl]sulfonyl]-1H-pyrazolo[4,3-b]pyridine. Grades: ≥98%. CAS No. 1642581-63-2. Molecular formula: C21H17N9O2S. Mole weight: 459.48.
Glutathionylspermidine disulfide
Glutathionylspermidine disulfide is an essential compound extensively employed in the biomedical sector, frequently harnessed as an efficacious antioxidant, effectively studying the detrimental impact of oxidative stress implicated in afflictions including cancer, neurodegenerative disorders and cardiovascular conditions. Synonyms: (2R)-2-amino-5-[[(2R)-1-[[2-[3-(4-aminobutylamino)propylamino]-2-oxoethyl]amino]-3-[[(2R)-3-[[2-[3-(4-aminobutylamino)propylamino]-2-oxoethyl]amino]-2-[[(4R)-4-amino-4-carboxybutanoyl]amino]-3-oxopropyl]disulfanyl]-1-oxopropan-2-yl]amino]-5-oxopentanoic acid. Molecular formula: C34H66N12O10S2. Mole weight: 867.09.
Glycine-β-muricholic Acid
Glycine-β-muricholic acid (GβMCA) is a potent, oral bioactive and intestine-selective antagonist of the farnesoid X receptor (FXR) that may be a candidate for the treatment of metabolic disorders. Synonyms: Gly-MCA; GβMCA; N-[(3α,5β,6β,7β)-3,6,7-trihydroxy-24-oxocholan-24-yl]-glycine; 5β-Cholanic acid-3α,6β,7β-triol N-(carboxymethyl)-amide. Grades: ≥95%. CAS No. 66225-78-3. Molecular formula: C26H43NO6. Mole weight: 465.63.
Glycyl-H 1152 dihydrochloride
Glycyl-H 1152 dihydrochloride is a glycyl analog of the Rho-kinase inhibitor H 1152 dihydrochloride with an improved selectivity for ROCKII (IC50 = 0.0118, 2.35, 2.57, 3.26, > 10 and >10 μM for ROCKII, Aurora A, CAMKII, PKG, PKA and PKC, respectively). Glycyl-H 1152 dihydrochloride is used for the treatment of hypertension and arteriosclerosis. Uses: The treatment of hypertension and arteriosclerosis. Synonyms: (S)-(+)-4-Glycyl-2-methyl-1-[(4-methyl-5-isoquinolinyl)sulfonyl]-hexahydro-1H-1,4-diazepine dihydrochloride; 2-amino-1-[(3S)-3-methyl-4-(4-methylisoquinolin-5-yl)sulfonyl-1,4-diazepan-1-yl]ethanone dihydrochloride. Grades: ≥99% by HPLC. CAS No. 913844-45-8. Molecular formula: C18H24N4O3S.2HCl. Mole weight: 449.4.
GM 1489
GM 1489 is a potent broad-spectrum inhibitor of matrix metalloproteinases (MMPs) with Ki values of 0.002, 0.1, 0.5, 0.2, and 20 μM for MMP-1, MMP-8, MMP-2, MMP-9, and MMP-3, respectively. Synonyms: Hexanoic acid, 3- [ [ [ (1S) -1- (1H-indol-3-ylmethyl) -2-oxo-2- [ [ (1S) -1-phenylethyl] amino] ethyl] amino] carbonyl] -5-methyl-, (3R)-; (3R) -3- [ [ [ (1S) -1- (1H-Indol-3-ylmethyl) -2-oxo-2- [ [ (1S) -1-phenylethyl] amino] ethyl] amino] carbonyl] -5-methylhexanoic acid; Hexanoic acid, 3-[[[1- (1H-indol-3-ylmethyl) -2-oxo-2-[ (1-phenylethyl) amino]ethyl]amino]carbonyl]-5-methyl-, [3R-[3R*[S*(S*)]]]-; GM-1489; GM1489. Grades: ≥98%. CAS No. 171347-75-4. Molecular formula: C27H33N3O4. Mole weight: 463.57.
GMC 1-116
GMC 1-116 is a metabolite of clozapine with weak 5-HT2 affinity and high M1 affinity (IC50 = 27 nM). Synonyms: 11-(4-Methyl-piperazin-1-yl)-5H-dibenzo[b,e][1,4]diazepin-8-ol; 8-Hydroxyclozapine; AC1L9SL1; 6-(4-methylpiperazin-1-yl)-5H-benzo[b][1,4]benzodiazepin-3-ol. Grades: 99%. CAS No. 63687-94-5. Molecular formula: C18H20N4O. Mole weight: 308.38.
GMC 1-165
GMC 1-165 is an analogue of clozapine with 5-HT2A/2C and hM1 receptor affinities. Synonyms: 11-(4-Methyl-piperazin-1-yl)-5H-dibenzo[b,e][1,4]diazepin-2-ol; 6-(4-methylpiperazin-1-yl)-11H-benzo[b][1,4]benzodiazepin-8-ol. Grades: 99%. CAS No. 156632-07-4. Molecular formula: C18H20N4O. Mole weight: 308.38.
GMC 1-169
GMC 1-169 is an atypical antipsychotic devoid of muscarinic activity. Uses: Atypical antipsychotic. Synonyms: [6-(4-methylpiperazin-1-yl)-11H-benzo[b][1,4]benzodiazepin-8-yl] trifluoromethanesulfonate. Grades: 99%. CAS No. 183140-97-8. Molecular formula: C19H19F3N4O3S. Mole weight: 440.44.
GMC 15-27
GMC 15-27 is a selective 5-HT1B/1D antagonist. Synonyms: 4'-(Aminoiminomethyl)-N-[4-methoxy-3-(4-methyl-1-piperazinyl)phenyl]-2'-methyl-[1,1'-biphenyl]-4-carboxamide. Grades: 98%. CAS No. 256227-71-1. Molecular formula: C27H31N5O2. Mole weight: 457.57.
GMC 2-113
GMC 2-113 is a selective 5-HT1B antagonist. Synonyms: BDBM50084961; ZINC13805066; N-[4-hydroxy-3-(4-methylpiperazin-1-yl)phenyl]-4-[2-methyl-4-(5-methyl-1,3,4-oxadiazol-2-yl)phenyl]benzamide. Grades: 98%. CAS No. 256227-77-7. Molecular formula: C28H29N5O3. Mole weight: 483.56.
GMC 2-118
GMC 2-118 is a potent and selective 5-HT1B antagonist. Synonyms: [4-[[4-[2-methyl-4-(5-methyl-1,3,4-oxadiazol-2-yl)phenyl]benzoyl]amino]-2-(4-methylpiperazin-1-yl)phenyl] methanesulfonate. Grades: 98%. CAS No. 256227-78-8. Molecular formula: C29H31N5O5S. Mole weight: 561.65.
GMC 2-29
GMC 2-29 is a potent and selective 5-HT1B/1D antagonist. Synonyms: N-[4-methoxy-3-(4-methylpiperazin-1-yl)phenyl]-4-[2-methyl-4-(5-methyl-1,3,4-oxadiazol-2-yl)phenyl]benzamide. Grades: 99%. CAS No. 148672-15-5. Molecular formula: C29H31N5O3. Mole weight: 497.59.
GMC 2-83
GMC 2-83 is an atypical antipsychotic without muscarinic activity. Uses: Atypical antipsychotic. Synonyms: [6-(4-methylpiperazin-1-yl)benzo[b][1,4]benzoxazepin-8-yl] trifluoromethanesulfonate. Grades: 99%. CAS No. 183140-98-9. Molecular formula: C19H18F3N3O4S. Mole weight: 441.42.
GMC 3-15
GMC 3-15 is a potent and selective 5-HT1B/1D antagonist. Synonyms: 4-[4-[[4-methoxy-3-(4-methylpiperazin-1-yl)phenyl]carbamoyl]phenyl]-3-methylbenzamide. Grades: 99%. CAS No. 691846-63-6. Molecular formula: C27H30N4O3. Mole weight: 458.55.
GNE-0877
GNE0877 is a highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitor with an IC50 of 3 nM. Synonyms: GNE0877; GNE 0877; GNE-0877. CAS No. 1374828-69-9. Molecular formula: C14H16F3N7. Mole weight: 339.326.
GNE-317
GNE-317 is a potent and selective PI3K inhibitor with potential anticncer activity. GNE-317 targets the PI3K pathway and can cross the Blood-Brain Barrier. GNE-317 was identified as having physicochemical properties predictive of low efflux by P-gp and BCRP. Studies in transfected MDCK cells showed that GNE-317 was not a substrate of either transporter. GNE-317 markedly inhibited the PI3K pathway in mouse brain, causing 40% to 90% suppression of the pAkt and pS6 signals up to 6-hour postdose. GNE-317 was efficacious in the U87, GS2, and GBM10 orthotopic models, achieving tumor growth inhibition of 90% and 50%, and survival benefit, respectively. GNE-317 could be effective in the treatment of GBM. Synonyms: GNE-317; GNE 317; GNE317. Grades: >98%. CAS No. 1394076-92-6. Molecular formula: C19H22N6O3S. Mole weight: 414.48.
GNE-477
GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor with IC50 of 4 nM for PI3Kα and Kiapp of 21 nM for mTOR. Synonyms: GNE-477, GNE477, GNE 477. Grades: >98%. CAS No. 1032754-81-6. Molecular formula: C21H28N8O3S2. Mole weight: 504.63.
GNE-493
GNE-493 is a potent, selective, and orally available dual pan-PI3K/mTOR inhibitor with IC50s of 3.4/12/16/16/32 nM for PI3Kα /PI3Kβ /PI3Kγ /PI3Kδ /mTOR respectively. Synonyms: GNE493; GNE-493; GNE 493. Grades: >98%. CAS No. 1033735-94-2. Molecular formula: C17H20N6O2S. Mole weight: 372.44.
GNE-4997
GNE-4997, a pyrazol derivative, has been found to be an ITK inhibitor that could have significant biological activities. Ki: 0.09 nM. Synonyms: GNE-4997; GNE-4997; GNE-4997; (4aS,5aR)-N-(1-((R)-((R)-1,1-dioxidotetrahydro-2H-thiopyran-2-yl)(phenyl)methyl)-1H-pyrazol-4-yl)-5,5-difluoro-5a-methyl-1,4,4a,5,5a,6-hexahydrocyclopropa[f]indazole-3-carboxamide. Grades: 98%. CAS No. 1705602-02-3. Molecular formula: C25H27F2N5O3S. Mole weight: 515.58.
GNE-617
GNE-617 is a novel and specific Nampt inhibitor with an IC50 of 18.9 nM in A549 cell. Synonyms: GNE-617; GNE 617; GNE617. Grades: >98%. CAS No. 1362154-70-8. Molecular formula: C21H15F2N3O3S. Mole weight: 427.42.
GNE-6468
GNE-6468, an imidazopyrimidine derivative, has been found to be a RORc inverse agonist that could be more effective than other members and be significant in studying the biological activities of RORC. Synonyms: GNE-6468; GNE 6468; GNE6468; 4-(6-(2-chloro-6-cyclopropylbenzoyl)imidazo[1,5-a]pyrimidin-8-yl)-2-hydroxybenzoic acid. Grades: 98%. CAS No. 1677668-27-7. Molecular formula: C23H16ClN3O4. Mole weight: 433.85.
GNE 9278
GNE 9278 is a positive allosteric modulator of NMDA receptors. GNE-9278 targets transmembrane domain (TMD) extracellular surface of agonist-bound NMDARs, stabilizing NMDARs in an activated state by slowing L-L-glu & gly off-rate. Synonyms: Benzenesulfonamide, 4-cyclohexyl-N-(1,7-dihydro-5-methyl-7-oxo-2-propyl[1,2,4]triazolo[1,5-a]pyrimidin-6-yl)-; GNE-9278; GNE9278; 4-cyclohexyl-N-(5-methyl-7-oxo-2-propyl-4,7-dihydro-[1,2,4]triazolo[1,5-a]pyrimidin-6-yl)benzenesulfonamide. Grades: ≥98% by HPLC. CAS No. 2315311-83-0. Molecular formula: C21H27N5O3S. Mole weight: 429.54.
GNE-9605
GNE-9605 retained excellent predicted human metabolic stability when assayed in human liver microsomes and hepatocytes. In addition, no reversible or time-dependent inhibition of any of the major CYP isoforms was observed. The demonstrated metabolic stability, brain penetration across multiple species, and selectivity of these inhibitors support their use in preclinical efficacy and safety studies. Synonyms: GNE9605; GNE-9605; GNE 9605. Grades: 0.98. CAS No. 1536200-31-3. Molecular formula: C17H20ClF4N7O. Mole weight: 449.839.
GNE-9822
GNE-9822, a pyrazole derivative, has been found to be a ITK inhibitor that could probably be effective in studies of some inflammatory disorders. Synonyms: GNE-9822; GNE 9822; GNE9822; (S)-N-[1-[3-(Dimethylamino)-1-phenylpropyl]-1H-pyrazol-4-yl]-6,6-dimethyl-4,5,6,7-tetrahydro-1H-indazole-3-carboxamide. Grades: 98%. CAS No. 1557232-32-2. Molecular formula: C24H32N6O. Mole weight: 420.56.
GNF1331
GNF1331 is a potent, selective and orally bioavailable porcupine (PORCN) inhibitor with IC50 value of 12 nM. It plays a critical role in multiple cancers, such as cutaneous squamous cell carcinoma (SCC), colorectal cancer and breast cancer. Uses: Gnf1331 plays a critical role in multiple cancers, such as cutaneous squamous cell carcinoma (scc), colorectal cancer and breast cancer. Synonyms: N-(6-methoxy-1,3-benzothiazol-2-yl)-2-[(4-propyl-5-pyridin-4-yl-1,2,4-triazol-3-yl)sulfanyl]acetamide; GNF-1331; GNF 1331; GNF1331. Grades: 98%. CAS No. 603101-22-0. Molecular formula: C20H20N6O2S2. Mole weight: 440.54.
GNF179
GNF179 exhibits a low clearance (CL=22 ml/min/kg, ~25% of hepatic blood flow in mice), a large volume of distribution (steady-state volume of distribution, Vss=11.8 l/kg), a moderate residence time (MRT=9 hours) and suitable terminal half-life (t1/2=8.9 hours). GNF179 reduced Plasmodium berghei parasitemia levels by 99.7% with a single 100 mg/kg oral dose, and prolonged mouse survival by an average of 19 days. GNF179 was able to protect against an infectious P. berghei sporozoite challenge with a single oral dose at 15 mg/kg while NITD609 was not. Synonyms: GNF 179; GNF-179. Grades: >98%. CAS No. 1261114-01-5. Molecular formula: C22H23ClFN5O. Mole weight: 427.9.
GNF-5
GNF-5 is the N-hydroxyethyl carboamide analog of GNF-2, a selective allosteric inhibitor of Bcr-Abl. GNF-5 demonstrates IC50 values of 4.52, 0.38, and 0.93 μM against Bcr-Abl mutants G250E, E255V, and M351T, respectively. Synonyms: GNF-5; GNF 5; GNF5. CAS No. 778277-15-9. Molecular formula: C20H17F3N4O3. Mole weight: 418.38.
GNF-7
GNF-7 is a type-II T315I inhibitor. GNF-7 inhibits Ack1 and germinal center kinase (GCK). GNF-7 is among the first type-II inhibitors capable of inhibiting T315I to be described and will serve as a valuable lead to design the third generation Bcr-Abl kinase inhibitors. Uses: Protein kinase inhibitors. Synonyms: GNF7; GNF 7; N-(4-methyl-3-(1-methyl-7-((6-methylpyridin-3-yl)amino)-2-oxo-1,4-dihydropyrimido[4,5-d]pyrimidin-3(2H)-yl)phenyl)-3-(trifluoromethyl)benzamide. Grades: 98%. CAS No. 839706-07-9. Molecular formula: C28H24F3N7O2. Mole weight: 547.54.
Golidocitinib
Golidocitinib is a novel potent and selective janus kinase 1 (JAK1) inhibitor, with antineoplastic properties. Synonyms: (2R)-N-(3-{2-[(3-methoxy-1-methyl-1H-pyrazol-4-yl)amino]pyrimidin-4-yl}-1H-indol-7-yl)-2-(4-methylpiperazin-1-yl)propanamide; AZD-4205; AZD4205; AZD 4205; NSC801813; NSC-801813; 1-Piperazineacetamide, N-(3-(2-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)-4-pyrimidinyl)-1H-indol-7-yl)-alpha,4-dimethyl-, (alphaR)-; JAK1 inhibitor 3; Golidocitinibum. Grades: ≥98%. CAS No. 2091134-68-6. Molecular formula: C25H31N9O2. Mole weight: 489.58.
Golotimod TFA
Golotimod TFA is an immunomodulating peptide that has antimicrobial activity. Golotimod TFA inhibits STAT3 signaling and modulates the duration and severity of oral mucositis in animal models that received radiation or a combination of radiation and Cisplatin. Synonyms: SCV 07 TFA. Molecular formula: C18H20F3N3O7. Mole weight: 447.36.
Gosogliptin
Gosogliptin is a dipeptidyl peptidase IV (DPP-IV) inhibitor. But no development was reported about Phase-II for Type-2 diabetes mellitus. Uses: Type 2 diabetes mellitus. Synonyms: UNII-GI718UO477; PF-00734200; PF 00734200; PF00734200; PF-734200; PF 734200; PF734200; CHEMBL515387;(3,3-difluoropyrrolidin-1-yl)-[(2S,4S)-4-(4-pyrimidin-2-ylpiperazin-1-yl)pyrrolidin-2-yl]methanone;89490-47-1(dihydrochloride). Grades: 98%. CAS No. 869490-23-3. Molecular formula: C17H24F2N6O. Mole weight: 366.42.