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This enzyme can also phosphorylate PtdIns3P in the 4-position, and PtdIns, PtdIns3P and PtdIns(3,4)P2 in the 5-position in vitro, but to a lesser extent. The last of these reactions occurs in vivo and is physiologically relevant. Three different isoforms are known. Group: Enzymes. Synonyms: diphosphoinositide kinase; PIP kinase; phosphatidylinositol 4-phosphate kinase; phosphatidylinositol-4-phosphate 5-kinase; type I PIP kinase. Enzyme Commission Number: EC 2.7.1.68. CAS No. 104645-76-3. Storage: Store it at +4 ?C for short term. For long term storage, store it at -20 ?C?-80 ?C. Form: Liquid or lyophilized powder. EXWM-3099; 1-phosphatidylinositol-4-phosphate 5-kinase; EC 2.7.1.68; 104645-76-3; diphosphoinositide kinase; PIP kinase; phosphatidylinositol 4-phosphate kinase; phosphatidylinositol-4-phosphate 5-kinase; type I PIP kinase. Cat No: EXWM-3099.
(2R,4S)-2-[(2S,5S)-5-(4-Hydroxyphenyl)-3,6-dioxo-2-piperazinyl]-5,5-dimethyl-4-thiazolidinecarboxylic Acid is an impurity in the synthesis of N-(Penicillan-6-yl) Open Ring Amoxicillinamide Disodium Salt , whch is an impurity of Amoxicillin (A634235); a semi-synthetic antibiotic related to Penicillin (P233500). Antibacterial. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 1mg, 2.5mg. Molecular Formula: C16H19N3O5S. US Biological Life Sciences.
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A 438079
A 438079 is a potent, and selective P2X 7 receptor antagonist with pIC 50 of 6.9. Uses: Scientific research. Group: Signaling pathways. CAS No. 899507-36-9. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-15488.
A 438079
A potent, competitive, and selective antagonist of P2X7 purinergic receptor (pIC50 = 6.5nM and 6.9nM for rat and human P2X7 receptor, respectively). Shown to reduce ATP-induced reactive oxygen species formation in MEL cells by about 87% (~10uM) and blocks BzATP-stimulated changes in intracellular calcium concentrations (IC50 = 100 and 300nM at rat and human P2X7 receptors, respectively. Developed by Abbott. Group: Biochemicals. Alternative Names: 3-((5-(2,3-dichlorophenyl)-1H-tetrazol-1-yl)methyl)pyridine Hydrochloride; P2X7 Purinergic Receptor Antagonist; A 438079; A438079; A-438079. Grades: Highly Purified. CAS No. 899507-36-9. Pack Sizes: 10mg. Molecular Formula: C??H?Cl?N? HCl, Molecular Weight: DMSO. US Biological Life Sciences.
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A 438079 hydrochloride
A 438079 hydrochloride is a competitive P2X7 receptor antagonist with pIC50 value of 6.9 for the inhibition of Ca2+ influx in the human recombinant P2X7 cell line. It protects against acetaminophen-induced liver injury by inhibiting p450 isoenzymes, but not by inflammasome activation. It partially but significantly prevented the 6-OHDA-induced depletion of striatal DA stores. Synonyms: 3-[[5-(2,3-Dichlorophenyl)-1H-tetrazol-1-yl]methyl]pyridine hydrochloride;A-438079 HCl;A-438079 hydrochloride; A438079 hydrochloride; A 438079 hydrochloride. Grades: >98 %. CAS No. 899507-36-9. Molecular formula: C13H10Cl3N5. Mole weight: 342.61.
A 438079 hydrochloride
A 438079 (hydrochloride) is a potent, and selective P2X 7 receptor antagonist with pIC 50 of 6.9. Uses: Scientific research. Group: Signaling pathways. CAS No. 899431-18-6. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-15488A.
A 438079 hydrochloride
Competitive P2X7 receptor antagonist (pIC50 = 6.9 for the inhibition of Ca2+ influx in the human recombinant P2X7 cell line). Devoid of activity at other P2 receptors (IC50 >> 10 μM). Possesses antinociceptive activity in models of neuropathic pain in vivo. Inhibits methamphetamine-induced microglial migration and phagocytosis in vitro. Group: Biochemicals. Alternative Names: 3-[[5-(2,3-Dichlorophenyl)-1H-tetrazol-1-yl]methyl]pyridine Monohydrochloride; 3-[[5-(2,3-Dichlorophenyl)-1H-tetrazol-1-yl]methyl]pyridine Monohydrochloride; A 438079. Grades: Highly Purified. CAS No. 899431-18-6. Pack Sizes: 10mg, 25mg. Molecular Formula: C??H??Cl?N?, Molecular Weight: 342.61. US Biological Life Sciences.
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AF 353
AF-353 is a novel, potent and orally bioavailable P2X3/P2X2/3 receptor antagonist. It is a highly potent inhibitor of α,β-meATP-evoked intracellular calcium flux in cell lines expressing recombinant rat and human P2X3 and human P2X2/3 channels. It also blocks human P2X2/3 channel function with marginally reduced potency (pIC50 = 7.3). It significantly reduces this parameter in both groups. It also reduces the inter-contractile interval in control but not in SCI rats. Synonyms: AF353; AF-353; 2,4-Pyrimidinediamine, 5-[5-iodo-4-Methoxy-2-(1-Methylethyl)phenoxy]-; Ro 4; 5-{[5-iodo-2-(1-Methylethyl)-4-(Methyloxy)phenyl]oxy}-2,4-pyrimidinediamine. Grades: >98%. CAS No. 865305-30-2. Molecular formula: C14H17IN4O2. Mole weight: 400.21.
An orally bioavailable sulfonamide compound that acts as a potent, reversible and allosteric y-secretase activity inhibitor with ~15-fold greater selectivity over Notch-1 proteolysis processing (IC50=7.1 and 105.9nM in HEK293-wtAPP) and preferentially inhibits PS1 (presenillin 1)-comprised y-secretase (EC50=8, 108, 286 and 29nM for PS1, Triple PS1-L172M,T281P, L282I, PS2 and Triple PS2-M178L, P287T, I288L), respectively). Shown to reduce the levels of Ab38, Ab40 and Ab42 in Tg2576 mice, Ab40 brain and plasma in APP-YAC mice (ED50=30 and 16mg/kg, p.o.) and Abtotal brain, CSF and plasma in guinea pigs (ED50=30mg/kg, i.p.). Group: Biochemicals. Grades: Highly Purified. CAS No. 290315-45-6. Pack Sizes: 5mg. US Biological Life Sciences.
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CAY10626
Phosphatidylinositol 3-kinases (PI3K) are a family of enzymes involved in cellular functions such as cell growth, proliferation, differentiation, motility, survival and intracellular trafficking, which in turn are involved in cancer. PI3K catalyzes the phosphorylation of the 3' hydroxyl position of PIs to produce PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3. CAY10626 demonstrates IC50 values of <3 and 13 nM for MDA361 (breast) and PC3 (prostate) cancer cell lines, respectively. Synonyms: CAY 10626; CAY-10626. Grades: ≥98%. CAS No. 1202884-94-3. Molecular formula: C31H35F3N8O3. Mole weight: 624.7.
GGTI-2418
GGTI-2418 is a synthetic peptidomimetic inhibitor of geranylgeranyltransferase I (GGTase I) that appears to induce apoptosis by downregulating several pivotal oncogenic and tumor survival pathways. GGTase I catalyzes the lipid posttranslational modification which is required for the function of Rho GTPases (frequently found aberrantly activated in human cancer). GGTase I inhibitors block Rho function in cancer cells and induce a G1 phase cell cycle arrest by a mechanism involving induction of the CDK inhibitors p21waf and p27kip, CDK2 and CDK4 inhibition and hypophoshorylation of the tumor suppressor Rb. GGTase I inhibitors also induce apoptosis by a mechanism involving downregulation of the expression of survivin and suppression of the activation of PI3K/Akt. Synonyms: GGTI 2418; GGTI-2418; GGTI 2418. CAS No. 501010-06-6. Molecular formula: C23H31N5O4. Mole weight: 441.532.
JTE-607 HCl
JTE-607, also known as TO-207, is a cytokine production inhibitor potentially for the treatment of systemic inflammatory response, and induces apoptosis accompanied by an increase in p21waf1/cip1 in acute myelogenous leukemia cells. Uses: Designed for use in research and industrial production. Additional or Alternative Names: TO-207; TO 207; TO207; JTE-607; JTE 607; JTE 607; JTE-607 HCl; JTE-607 dihydrochloride. Product Category: Inhibitors. Appearance: Solid powder. CAS No. 188791-09-5. Molecular formula: C25H33Cl4N3O5. Mole weight: 597.36. Purity: >98%. IUPACName: N-[3,5-Dichloro-2-hydroxy-4-[2-(4-methyl-1-piperazinyl)ethoxy]benzoyl]-L-phenylalanine ethyl ester dihydrochloride. Canonical SMILES: O=C(OCC)[C@H](CC1=CC=CC=C1)NC(C2=CC(Cl)=C(OCCN3CCN(C)CC3)C(Cl)=C2O)=O.[H]Cl.[H]Cl. Product ID: ACM188791095. Alfa Chemistry ISO 9001:2015 Certified.
MRS 2211
MRS 2211 is a competitive P2Y13 receptor antagonist (pIC50 = 5.97), with > 20-fold selectivity over P2Y1 and P2Y12 receptors. It is known that MRS 2211 inhibits ADP-induced inositol trisphosphate (IP3) formation. Research suggests that MRS 2211 inhibits phospholipase C (PLC) response to 2-methylthio-ADP in 1321N1 astrocytoma cells. Synonyms: 2-[(2-Chloro-5-nitrophenyl)azo]-5-hydroxy-6-methyl-3-[(phosphonooxy)methyl]-4-pyridinecarboxaldehyde disodium salt; MRS2211; MRS-2211. Grades: ≥96% by HPLC. Molecular formula: C14H10N4O8Na2PCl. Mole weight: 474.66.
N6-(6-Amino)hexyl-ATP - ATTO-465
N6-(6-Amino)hexyl-ATP - ATTO-465, a powerful fluorescent dye labeled ATP analog expertly employed in functional signaling assays to effectively track protein activity or ATP consumption inside functioning cells. Additionally, this steadfast compound acts as a robust agonist of P2X receptors, widely utilized in conducting pioneering neurological disease investigations such as those delving into the enigmatic pathologies of Alzheimer's and Parkinson's disease, where it has proven itself as an indispensable research tool of incomparable quality. Synonyms: N; -(6-Amino)hexyl-adenosine-5'-triphosphate, labeled with ATTO 465, Triethylammonium salt. Grades: ≥ 95 % by HPLC. Molecular formula: C33H44N9O14P3(free acid). Mole weight: 883.68 (free acid).
P2X Antagonist III (Purinergic Receptor P2X Antagonist III, N- ( (4- (4-Phenylpiperazin-1-yl) tetrahydro-2H-pyran-4-yl) methyl) -2- (phenylthio) nicotinamide)
A phenylthio-nicotinamide that acts as a high affinity P2X7 antagonist (pKi = 8.7 and 7.9, respectively, against 30nM A-804598 for rat and human P2X7 binding) and potently inhibits P2X7-dependent cellular Ca2+ mobilization (pIC50 = 8.3, 7.5, and 7.2, respectively, using 1321N1 expressing human, mouse, or rat P2X7; drug added 0.5 h prior to 3 min 0.25 mM BzATP stimulation), while exhibiting much reduced or little potency toward a panel of 50 ion channels, transporters, and receptors. Although not suitable for oral dosing due to high hepatic extraction ratios, effective delivery and brain P2X7 occupancy can be achieved via s.c. dosing in rats (30mg/kg) in vivo. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences.
This enzyme hydroylses 1-phosphatidyl-1D-myo-inositol 3,4,5-trisphosphate (PtdIns(3,4,5)P3) to produce PtdIns(3,4)P2, thereby negatively regulating the PI3K (phosphoinositide 3-kinase) pathways. The enzyme also shows activity toward (PtdIns(1,3,4,5)P4). The enzyme is involved in several signal transduction pathways in the immune system leading to an adverse range of effects. Group: Enzymes. Synonyms: SHIP1; SHIP2; SHIP; p150Ship. Enzyme Commission Number: EC 3.1.3.86. Storage: Store it at +4 ?C for short term. For long term storage, store it at -20 ?C?-80 ?C. Form: Liquid or lyophilized powder. EXWM-3692; phosphatidylinositol-3,4,5-trisphosphate 5-phosphatase; EC 3.1.3.86; SHIP1; SHIP2; SHIP; p150Ship. Cat No: EXWM-3692.
phosphoinositide phospholipase C
These enzymes form some of the cyclic phosphate Ins(cyclic1,2)P(4,5)P2 as well as Ins(1,4,5)P3. They show activity towards phosphatidylinositol, i.e., the activity of EC 4.6.1.13, phosphatidylinositol diacylglycerol-lyase, in vitro at high [Ca2+]. Four β-isoforms regulated by G-proteins, two γ-forms regulated by tyrosine kinases, four Δ-forms regulated at least in part by calcium and an ε-form, probably regulated by the oncogene ras, have been found. Group: Enzymes. Synonyms: triphosphoinositide phosphodiesterase; phosphoinositidase C; 1-phosphatidylinositol-4,5-bisphosphate phosphodiesterase; monophosphatidylinositol phosphodiesterase; phosphatidylinositol phospholipase C; PI-PLC; 1-phosphatidyl-D-myo-inositol-4,5-bisphosphate inositoltrisphosphohydrolase. Enzyme Commission Number: EC 3.1.4.11. CAS No. 63551-76-8. Storage: Store it at +4 ?C for short term. For long term storage, store it at -20 ?C?-80 ?C. Form: Liquid or lyophilized powder. EXWM-3711; phosphoinositide phospholipase C; EC 3.1.4.11; 63551-76-8; triphosphoinositide phosphodiesterase; phosphoinositidase C; 1-phosphatidylinositol-4,5-bisphosphate phosphodiesterase; monophosphatidylinositol phosphodiesterase; phosphatidylinositol phospholipase C; PI-PLC; 1-phosphatidyl-D-myo-inositol-4,5-bisphosphate inositoltrisphosphohydrolase. Cat No: EXWM-3711.
The human p27Kip1 C-terminus PIM-1 phosphorylation site- (Thr198) containing sequence is synthesized with an N-terminal Arg octamer/R8-containing sequence to facilitate its use as a cell-permeable, substrate-competitive PIM-1 inhibitor. Reported to completely prevents human prostate carcinoma DU145-derived tumor expansion for up to 17 days (0.5umol/animal on days 0 & 5; intratumoral injection) in mice in vivo when combined with a single Taxol dosage on day zero (60mg/kg; i.p.). Studies using FITC-conjugated R8-T198wt demonstrate that R8-T198wt-induced cell cycle arrest and apoptosis in PIM-1-expressing DU145 cells are direct consequences of inhibition of PIM-1-mediated p27Kip1 Thr198 and Bad Ser112 phosphorylation, respectively. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 5mg. US Biological Life Sciences.
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PIT
PIT selectively and non-competitively blocked P2Y1 receptor signaling without affecting nucleotide binding. PIT had no significant effect on agonist activation of other P2Y receptors, including P2Y2, P2Y4, P2Y6, P2Y11 and P2Y12 receptors. Synonyms: 2-(2-Pyridinyl)-(3H)-indol-3-one-1-oxide 4-methylbenzenesulfonate; 2,2'-Pyridylisatogen tosylate. Grades: ≥99% by HPLC. CAS No. 56583-49-4. Molecular formula: C13H8N2O2.C7H8O3S. Mole weight: 396.42.
p-nitro-Pifithrin-α
p-nitro-Pifithrin-α is a cell-permeable p53 inhibitor. It blocks p53-mediated expression of p21/WAF1 and apoptosis in cortical neurons ten-fold more potently than pifithrin-&alpha. It also suppresses p53-mediated TGF-β1 expression in human proximal tubular cells and attenuates steatosis and liver injury in mice fed a high-fat diet. Synonyms: p-nitro-PFT-α; 2-(2-imino-4,5,6,7-tetrahydro-1,3-benzothiazol-3-yl)-1-(4-nitrophenyl)ethanone hydrobromide. Grades: ≥95%. CAS No. 389850-21-9. Molecular formula: C15H15N3O3S·HBr. Mole weight: 398.3.
PPTN hydrochloride
PPTN, a 4,7-disubstituted 2-naphthoic acid derivative, is a high affinity and selective P2Y14 antagonist (KB = 434 pM) with >10,000-fold selectivity for P2Y14 over other P2Y receptors. PPTN blocks UDP-glucose-promoted chemotaxis of human neutrophils and does so across a concentration range consistent with its KB determined in the P2Y14-R-expressing cell line. Synonyms: 4-[4-(4-Piperidinyl)phenyl]-7-[4-(trifluoromethyl)phenyl]-2-naphthalenecarboxylic acid hydrochloride. Grades: ≥98% by HPLC. CAS No. 1992047-65-0. Molecular formula: C29H24F3NO2.HCl. Mole weight: 511.96.
RO-3
RO-3 is a potent, CNS-penetrant, and orally active P2X 3 and P2X 2/3 antagonist with pIC 50 s of 5.9 and 7.0 for human homomultimeric P2X 3 and heteromultimeric P2X 2/3 receptors, respectively. RO-3 shows selectivity for P2X 3 and P2X 2/3 over all other functional homomultimeric P2X receptors (IC 50 >10 μM at P2X 1,2,4,5,7 ) [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 1026582-88-6. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg. Product ID: HY-19978.
RO-3
RO-3 is a selective homomeric P2X3 and heteromeric P2X2/3 receptor antagonist (pIC50 values are 7.0 and 5.9 respectively). RO-3 is used in a combination of compounds to develop a substance used for alleviating pain and skin disorders. Synonyms: 5-[[4,5-Dimethoxy-2-(methylethyl)phenyl]methyl]-2,4-pyrimidinediamine; RO-3; RO 3; RO3. Grades: ≥98% by HPLC. CAS No. 1026582-88-6. Molecular formula: C16H22N4O2. Mole weight: 302.37.
Ro 51
Ro 51 is a potent and selective dual antagonist of purinoceptor subtypes P2X3 and P2X2/3 (IC50 values are 2 and 5 nM for rP2X3 and hP2X2/3 respectively), without significant activity on other P2X receptors (IC50 values are > 10 μM for P2X1, P2X2, P2X4, P2X5, and P2X7). P2X3 and P2X2/3 have been shown to play a pivotal role in models of various pain conditions making Ro 51 a potential option in the treatment of pain. Synonyms: 2-[[4-Amino-5-[5-iodo-4-methoxy-2-(1-methylethyl)phenoxy]-2,4-pyrimidinyl]amino]-1,3-propanediol; Ro51; Ro-51; CHEMBL494161; 1050670-85-3; SCHEMBL4970553. Grades: ≥98% by HPLC. CAS No. 1050670-85-3. Molecular formula: C17H23IN4O4. Mole weight: 474.29.
Ro 51
Ro 51 is a potent and selective dual antagonist of purinoceptor subtypes P2X3 and P2X2/3. P2X3 and P2X2/3 have been shown to play a pivotal role in models of various pain conditions making Ro 51 a potential option in the treatment of pain. Group: Biochemicals. Alternative Names: 2-[[4-Amino-5-[5-iodo-4-methoxy-2-(1-methylethyl)phenoxy]-2-pyrimidinyl]amino]-1,3-propanediol; RO-51. Grades: Highly Purified. CAS No. 1050670-85-3. Pack Sizes: 10mg. US Biological Life Sciences.
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SAR 216471 hydrochloride
SAR 216471 hydrochloride is a potent and reversible P2Y12 antagonist (IC50 = 17 nM), displaying antiplatelet and antithrombotic activity in vivo. Synonyms: SAR 216471 hydrochloride; SAR-216471 hydrochloride; SAR216471 hydrochloride; 5-Chloro-N-[6-[5-methyl-4-(1-oxobutyl)-1H-pyrazol-1-yl]-3-pyridazinyl]-1-[2-(4-methyl-1-piperazinyl)-2-oxoethyl]-1H-indole-3-carboxamide hydrochloride. Grades: ≥98% by HPLC. CAS No. 1279829-64-9. Molecular formula: C28H31ClN8O3.HCl. Mole weight: 599.51.
SMI-4a
Selective inhibitor of Pim-1 and Pim-2 protein kinases. Inducer of G1 phase cell cycle arrest. Inducer of p27Kip1. Inducer of apoptosis through the mitochondrial pathway. Inhibitor of the mammalian target of rapamycin C1 (mTORC1) pathway. Downregulates c-myc. Inhibitor of PRAS40 phosphorylation and mTOR activity. Potential anti-cancer compound. Blocks prostate cancer growth. Group: Biochemicals. Grades: Highly Purified. CAS No. 327033-36-3. Pack Sizes: 5mg. Molecular Formula: C11H6F3NO2S, Method for Determining. US Biological Life Sciences.
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TC-P 262
TC-P 262 is a selective P2X3 and P2X2/3 receptor antagonist (pIC50 = 7.39 and 6.68, respectively). TC-P 262 has no detectable activity at P2X1, P2X2, P2X4 and P2X7 receptors (pIC50 < 4.7). Synonyms: 5-[5-Methyl-2-(1-methylethyl)phenoxy]-2,4-pyrimidinediamine. Grades: ≥99% by HPLC. CAS No. 873398-67-5. Molecular formula: C14H18N4O. Mole weight: 258.32.
A membrane permeable dihydroquinolinyloxo-isoindolinedione compound that acts as a potent and selective agonist of lysosomal mucolipin transient receptor potential (TRP) channel 1,2,3 (TRPML) in all mammalian cells. Does not appear to affect six other related TRP channels. Shown to rapidly activate whole-endolysosome TRPML-like current and induce lysosomal Ca2+ release (~10uM). Its activating action on whole-endolysosome is comparable to that of PI(3,5)P2 (1uM) with which it shows a synergistic effect. ML-SA1-induced Ca2+ responses are reportedly abolished by glycyl-L-phenylalanine 2-naphthylamide, induces osmotic lysis of lysosomes, and Bafilomycin A1, a V-ATPase inhibitor. Also reduces lactosylceramide and cholesterol accumulation and corrects trafficking defects in Niemann-Pick (NP) disease cells. Group: Biochemicals. Grades: Highly Purified. CAS No. 332382-54-4. Pack Sizes: 25mg. US Biological Life Sciences.
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TTA-P2
TTA-P2 is a selective T-type calcium channel blocker. It blocks T-type currents with an IC50 of 100 nM and stabilized channel in the inactive state in rats DRGs. TTA-P2 potentially acts as an antinociceptive and an antiinflammatory agent. Synonyms: TTA-P2; TTA P2; TTAP2; (S)-3,5-Dichloro-N-((1-((2,2-dimethyltetrahydro-2H-pyran-4-yl)methyl)-4-fluoropiperidin-4-yl)methyl)benzamide; CHEMBL488817; 3,5-dichloro-N-[[4-fluoro-1-[[(4S)-tetrahydro-2,2-dimethyl-2H-pyran-4-yl]methyl]-4-piperidinyl]methyl]Benzamide; 3,5-Dichloro-N-[(1-{[(4S)-2,2-dimethyloxan-4-yl]methyl}-4-fluoropiperidin-4-yl)methyl]benzamide. CAS No. 1072018-68-8. Molecular formula: C21H29Cl2FN2O2. Mole weight: 431.373.
YM-201636
YM201636 is an inhibitor of retroviral budding and PIKfyve-catalyzed PtdIns(3,5)P2 synthesis, can halt glucose entry by insulin in adipocytes. YM201636 almost completely inhibited basal and insulin-activated 2-deoxyglucose uptake at doses as low as 160 nM, with IC(50)=54+/-4 nM for the net insulin response. Insulin-induced GLUT4 translocation was partially inhibited at substantially higher doses, comparable to those required for inhibition of insulin-induced phosphorylation of Akt/PKB. In addition to PIKfyve, YM201636 also completely inhibited insulin-dependent activation of class IA PI 3-kinase. Synonyms: YM 201636; YM201636. Grades: >98%. CAS No. 371942-69-7. Molecular formula: C25H21N7O3. Mole weight: 467.48.
A novel, potent, orally bioavailable antagonist of P2X3/P2X2/3 receptors (pIC50 = 8 in human and rat; pIC50 = 7.3 for human P2X2/3 receptor). Shown to be highly brain penetrant with a brain to plasma ratio of 6. Blocks agonist-evoked intracellular Ca2+ flux and inward currents in nanomolar range (10nM to 1uM) in cell lines recombinantly expressing human P2X3 and P2X2/3 receptors. Exhibits desirable pharmacokinetic properties (t1/2 = 1.63 h and Tmax = 30 min). Group: Biochemicals. Grades: Highly Purified. CAS No. 927887-18-1. Pack Sizes: 5mg. Molecular Formula: C??H??ClIN?O?. US Biological Life Sciences.
A highly selective and competitive antagonist of P2Y13 purinergic receptor (pIC50 = 5.97). Exhibits about 20-fold greater selectivity over P2Y1 and P2Y12 receptors. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. US Biological Life Sciences.
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