Cyp3a4 Suppliers USA
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Product | Description | |
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16α-Hydroxy estrone Quick inquiry Where to buy Suppliers range | 16α-Hydroxy estrone is a hydroxylated metabolite of E1 as well as an interconversion product with E2. E1 is 16α-hydroxylated by cytochrome P450 (CYP) isoforms, including CYP1A1, CYP3A5, CYP3A4, and CYP3A7, with CYP3A5 being breast-specific. Synonyms: 16α-OHE1; 16a-Hydroxyestrone. Grades: ≥98%. CAS No. 566-76-7. Molecular formula: C18H22O3. Mole weight: 286.4. | |
[1(S)-Phenylethoxy]-Aprepitant Quick inquiry Where to buy Suppliers range | [1(S)-Phenylethoxy]-Aprepitant is a derivative of Aprepitant (A729800), a novel selective neurokinin-1 (NK-1) receptor antagonist. In vitro studies using human liver microsomes indicate that Aprepitant is metabolised primarily by CYP3A4 with minor metabolism by CYP1A2 and CYP2C19, and no metabolism by CYP2D6, CYP2C9, or CYP2E1. Group: Biochemicals. Grades: Highly Purified. CAS No. 170902-81-5. Pack Sizes: 1mg, 10mg. Molecular Formula: C23H21F7N4O3, Molecular Weight: 534.429999999999. US Biological Life Sciences. | Worldwide |
(2R,3R,1S)-Aprepitant Quick inquiry Where to buy Suppliers range | (2R,3R,1S)-Aprepitant is an impurity of Aprepitant (A729800); a novel selective neurokinin-1 (NK-1) receptor antagonist. In vitro studies using human liver microsomes indicate that Aprepitant is metabolised primarily by CYP3A4 with minor metabolism by CYP1A2 and CYP2C19, and no metabolism by CYP2D6, CYP2C9, or CYP2E1. Antiemetic. Group: Biochemicals. Grades: Highly Purified. CAS No. 1242175-34-3. Pack Sizes: 1mg. Molecular Formula: C23H21F7N4O3, Molecular Weight: 534.429999999999. US Biological Life Sciences. | Worldwide |
(2S,3R,1R)-Aprepitant Quick inquiry Where to buy Suppliers range | (2S,3R,1R)-Aprepitant is an impurity of Aprepitant (A729800); a novel selective neurokinin-1 (NK-1) receptor antagonist. In vitro studies using human liver microsomes indicate that Aprepitant is metabolised primarily by CYP3A4 with minor metabolism by CYP1A2 and CYP2C19, and no metabolism by CYP2D6, CYP2C9, or CYP2E1. Antiemetic. Group: Biochemicals. Grades: Highly Purified. CAS No. 1185502-97-9. Pack Sizes: 1mg, 2.5mg. Molecular Formula: C23H21F7N4O3, Molecular Weight: 534.429999999999. US Biological Life Sciences. | Worldwide |
(2S,3S,1R)-Aprepitant Quick inquiry Where to buy Suppliers range | (2S,3S,1R)-Aprepitant is an impurity of Aprepitant (A729800); a novel selective neurokinin-1 (NK-1) receptor antagonist. In vitro studies using human liver microsomes indicate that Aprepitant is metabolised primarily by CYP3A4 with minor metabolism by CYP1A2 and CYP2C19, and no metabolism by CYP2D6, CYP2C9, or CYP2E1. Antiemetic. (2S,3S,1R)-Aprepitant is also a useful synthetic intermediate in the synthesis of morpholine tachykinin receptor antagonist prodrugs. Group: Biochemicals. Grades: Highly Purified. CAS No. 172822-28-5. Pack Sizes: 1mg. Molecular Formula: C23H21F7N4O3, Molecular Weight: 534.429999999999. US Biological Life Sciences. | Worldwide |
4',5'-Dihydro-8-Hydroxy Psoralen Quick inquiry Where to buy Suppliers range | 4',5'-Dihydro-8-hydroxypsoralen is a furancouramin with inhibitory activity on CYP3A4 as well as inhibitory effects on prostaglandin E2 production. 4',5'-Dihydro-8-hydroxypsoralen is an impurity of 8-Methoxypsoralen , also known as Methoxsalen. Group: Biochemicals. Alternative Names: 2,3-Dihydro-9-hydroxy-7H-furo[3,2-g][1]benzopyran-7-one; 2,3-Dihydro-6,7-dihydroxy-5-benzofuranacrylic Acid δ-Lactone; 2,3-Dihydroxanthotoxol. Grades: Highly Purified. CAS No. 68123-30-8. Pack Sizes: 25mg. US Biological Life Sciences. | Worldwide |
6,7-Dihydroxy bergamottin Quick inquiry Where to buy Suppliers range | 6,7-Dihydroxy bergamottin (6,7-DHB) is a potent inhibitor of CYP3A4 (IC50 = 25 μM). Uses: Cytochrome p-450 enzyme inhibitors. Synonyms: 6,7-DHB; 6,7-dihydroxybergamottin. Grades: ≥98%. CAS No. 145414-76-2. Molecular formula: C21H24O6. Mole weight: 372.4. | |
6',7'-Epoxybergamottin Quick inquiry Where to buy Suppliers range | 6'7'-Epoxybergamottin is a furanocoumarin found in grapefruit. It is a potent inhibitor of the cytochrome P450 (CYP) isoform CYP3A4 with an IC50 value of 0.30 ppm in a cell-free assay, 0.33 μM in HL7 human liver cells, and 0.22 μM in S9 human intestine cells. Synonyms: Epoxybergamottin; 4-[(E)-5-(3,3-dimethyloxiran-2-yl)-3-methylpent-2-enoxy]furo[3,2-g]chromen-7-one. Grades: ≥98%. CAS No. 206978-14-5. Molecular formula: C21H22O5. Mole weight: 354.4. | |
6β-Hydroxycortisone Quick inquiry Where to buy Suppliers range | 6β-Hydroxycortisone can be used as a probe to detect inhibition of CYP3A4 in vivo. Synonyms: (6β)-6,17,21-Trihydroxy-pregn-4-ene-3,11,20-trione; 11-Dehydro-6β,17-dihydroxy-corticosterone; 6β,17,21-Trihydroxy-pregn-4-ene-3,11,20-trione; 6β,17α,21-Trihydroxy-4-pregnene-3,11,20-trione; NSC 15457. Grades: > 95%. CAS No. 16355-28-5. Molecular formula: C21H28O6. Mole weight: 376.44. | |
Alectinib Quick inquiry Where to buy Suppliers range | Alectinib, marketed as Alecensa, is an oral drug that blocks the activity of anaplastic lymphoma kinase (ALK) and is used to treat non-small-cell lung cancer (NSCLC). Alectinib has a low potential for interactions. While it is metabolised by the liver enzyme CYP3A4, and blockers of this enzyme accordingly increase its concentrations in the body, they also decrease concentrations of the active metabolite M4, resulting in only a small overall effect. Conversely, CYP3A4 inducers decrease alectinib concentrations and increase M4 concentrations. Interactions via other CYP enzymes and transporter proteins cannot be excluded but are unlikely to be of clinical significance. Synonyms: CH-5424802; CH5424802; CH 5424802; AF-802; RG-7853; RO5424802. Grades: ≥95%. CAS No. 1256580-46-7. Molecular formula: C30H34N4O2. Mole weight: 482.62. | |
Asiaticoside Quick inquiry Where to buy Suppliers range | Antibacterial. Human collagen I synthesis inducer. Anti-wrinkle activity. Shows wound healing activity. Enhances normal human skin cell migration, attachment and growth. Suppresses collagen expression and TGF-beta/Smad signaling by inducing Smad7 and inhibiting TGF-betaRI and TGF-betaRII. Anti-inflammatory. Anti-gastric ulcer. Mitogen-activated protein kinases (MAPKs), nuclear factor-kappaB (NF-kappaB), cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS; NOSII) expression, production of serum tumor necrosis factor (TNF-alpha) and interleukin-6 (IL-6) inhibitor. Apoptosis inducer in cancer cells. Enhances antitumor activity of vincristine in cancer cells. Might be useful in cancer chemotherapy. Anxiolytic. Antidepressant-like activity. Hepatoprotective effects. CYP2C19 and CYP3A4 inhibitor. Neuroprotective. Antileishmanial activity. cPLA2 and sPLA2 inhibitor. Group: Biochemicals. Alternative Names: Blastostimulina, Centelase, Emdecassol, Madecassol, Marticassol, FK1080, BRN 0078195, NSC 166062. Grades: Highly Purified. CAS No. 16830-15-2. Pack Sizes: 10mg, 50mg. Molecular Formula: C48H78O19. US Biological Life Sciences. | Worldwide |
Avanafil metabolite M4 Quick inquiry Where to buy Suppliers range | Avanafil metabolite M4 is a major active metabolite of the phosphodiesterase 5 (PDE5) inhibitor avanafil. Avanafil is metabolized by the cytochrome P450 (CYP450) isoforms CYP3A4 and CYP2C to the major metabolites avanafil metabolite M4 and avanafil metabolite M16, as well as minor metabolites. Avanafil metabolite M4 inhibits PDE5 with 18% of the potency of avanafil. Grades: ≥98%. Molecular formula: C23H26ClN7O4. Mole weight: 499.95. | |
Azamulin Quick inquiry Where to buy Suppliers range | Highly selective human CYP3A4 inhibitor. A mutilin derivative. Group: Biochemicals. Alternative Names: 14-O- (5- (2-Amino1, 3, 4-triazolyl) thioacetyl) dihydromutilin; Antibiotic TDM 85-530; SA 85530b; (5-Amino-1H-1,2,4-triazol-3-yl)thio]acetic acid (3aS, 4R, 5S, 6R, 8R, 9R, 9aR, 10R)-6-ethyldecahydro-5-hydroxy-4, 6, 9, 10-tetramethyl-1-oxo-3a, 9-propano-3aH-cyclopentacycloocten-8-yl ester. Grades: Highly Purified. CAS No. 76530-44-4. Pack Sizes: 5mg. US Biological Life Sciences. | Worldwide |
Bergaptol Quick inquiry Where to buy Suppliers range | A hydroxylated psoralen that acts as a potent inhibitors of debenzylation activity of CYP3A4 enzyme with an IC50 value of 24.92 and 42.93 μM, respectively. Recent studies suggest that it may have antiproliferative and anticancer properties. Group: Biochemicals. Alternative Names: 4-Hydroxy-7H-furo[3,2-g][1]benzopyran-7-one; 4-Hydroxybergapten; 5-Hydroxy-6,7-furanocoumarin; 5-Hydroxypsoralen; NSC 341958. Grades: Highly Purified. CAS No. 486-60-2. Pack Sizes: 25mg. US Biological Life Sciences. | Worldwide |
BMS-582949 hydrochloride Quick inquiry Where to buy Suppliers range | BMS-582949 hydrochloride is a potent and selective P38 mitogen-activated protein kinase (P38 MAPK) inhibitor with IC50 of 13 nM. It displays >2000-fold selectivity for p38α over a diverse panel of 57 kinases including serine kinases, nonreceptor tyrosine kinases, receptor tyrosine kinases, and the p38γ and δ isoforms. It is a weak inhibitor of CYP3A4, with an IC50 value ranging from 18 to 40 μM based in multiple tests. It does not significantly inhibit cytochrome P450 isozymes 1A2, 2C9, 2C19, and 2D6 in vitro. It exhibited oral bioavailability values of 90% and 60% in mice and rats, respectively. It is currently under Phase II clinical trials for the treatment of inflammatory diseases. Uses: Bms-582949 hydrochloride is used for the treatment of inflammatory diseases. Synonyms: BMS 582949 hydrochloride; BMS582949 hydrochloride; BMS-582949 hydrochloride; 4-((5-((Cyclopropylamino)carbonyl)-2-methylphenyl)amino)-5-methyl-n-propylpyrrolo(2,1-f)(1,2,4)triazine-6-carboxamide. Grades: >98%. CAS No. 912806-16-7. Molecular formula: C22H27ClN6O2. Mole weight: 442.94. | |
BMS695735 Quick inquiry Where to buy Suppliers range | BMS695735 is a benzimidazole inhibitor of the insulin-like growth factor-1 receptor. It was also found to have potent CYP3A4 inhibition. It has broad spectrum in vivo antitumor activity. Uses: Bms695735 has broad spectrum antitumor activity. Synonyms: BMS-695735; BMS 695735; BMS695735; CHEMBL459729; BDBM27888; DNC008930; 2(1H)-Pyridinone, 4-((2-(4-chloro-1H-pyrazol-1-yl)ethyl)amino)-3-(5-(1-(3-fluoropropyl)-4-piperidinyl)-7-methyl-1H-benzimidazol-2-yl)-;(3Z)-4-[2-(4-chloropyrazol-1-yl)ethylamino]-3-[6-[1-(3-fluoropropyl)piperidin-4-yl]-4-methyl-1,3-dihydrobenzimidazol-2-ylidene]pyridin-2-one. Grades: 95%. CAS No. 1054315-48-8. Molecular formula: C26H31ClFN7O. Mole weight: 512.02. | |
Cedrol Quick inquiry Where to buy Suppliers range | Cedrol is a bioactive sesquiterpene, a potent competitive inhibitor of cytochrome P-450 (CYP) enzymes. Cedrol inhibits CYP2B6-mediated bupropion hydroxylase and CYP3A4-mediated midazolam hydroxylation with Ki of 0.9 μM and 3.4 μM, respectively. Cedrol also has weak inhibitory effect on CYP2C8, CYP2C9, and CYP2C19 enzymes. Cedrol is found in cedar essential oil and poetesses anti-septic, anti-inflammatory, anti-spasmodic, tonic, astringent, diuretic, insecticidal, and anti-fungal activities. Group: Biobased Products. Alternative Names: Cypress camphor. Grades: 99%. CAS No. 77-53-2. Product ID: BBC77532. Molecular formula: C15H26O. Mole weight: 222.37. IUPAC Name: (1S, 2R, 5S, 7R, 8R)-2, 6, 6, 8-Tetramethyltricyclo[5.3.1.01, 5]undecan-8-ol. Appearance: Pale yellow to yellow green solid. Density: 0.9479 g/cm³. SMILES: CC1CCC2C13CCC(C(C3)C2(C)C)(C)O. | |
Cobicistat Quick inquiry Where to buy Suppliers range | Cobicistat is a potent inhibitor of cytochrome P450 3A enzymes, including the important CYP3A4 subtype. It also inhibits intestinal transport proteins, increasing the overall absorption of several HIV medications, including atazanavir, darunavir and tenofovir alafenamide fumarate. Uses: Anti-hiv agents. Synonyms: Cobicistat, GS-9350; GS 9350; GS9350. Grades: 0.99. CAS No. 1004316-88-4. Molecular formula: C40H53N7O5S2. Mole weight: 776.028. | |
CYP3cide Quick inquiry Where to buy Suppliers range | CYP3cide is a potent and selective time dependent inactivator of Cytochrome P450 3A4 (CYP3A4). CYP3A4 is an important enzymes involved in the metabolism of xenobiotics in the human body and constitutes to about a quarter of all CYPs in the human body. CYP3cide provides a useful in vitro tool in defining the individual roles of CYP3A4 versus CYP3A5 in the metabolism of drugs. Group: Biochemicals. Alternative Names: PF-04981517. Grades: Highly Purified. CAS No. 1390637-82-7. Pack Sizes: 10mg. US Biological Life Sciences. | Worldwide |
Ellipticine (NSC 71795) Quick inquiry Where to buy Suppliers range | Ellipticine is an alkaloid isolated from Apocyanaceae plants that exhibits antitumor activities by intercalating into DNA and/or inhibiting DNA topoisomerase II. It forms covalent adducts in DNA after being enzymatically activated with cytochrome P450 isoforms (e.g., CYP3A4, CYP1A1, or CYP1A2) or by peroxidases in target tissues. Ellipticine has been shown to inhibit the proliferation of human breast adenocarcinoma MCF-7 cells, leukemia HL-60 and CCRF-CEM cells, neuroblastoma IMR-32, UKF-NB-3, and UKF-NB-4 cells, and U87MG glioblastoma cells with IC50 values ranging from 0.27-4.7uM. Group: Biochemicals. Alternative Names: 5,11-dimethyl-6H-pyrido[4,3-b]carbazole, NSC 71795. Grades: Highly Purified. CAS No. 519-23-3. Pack Sizes: 5mg, 10mg, 25mg, 50mg. Molecular Formula: C17H14N2, Molecular Weight: 246.3. US Biological Life Sciences. | Worldwide |
GSK 962040 Quick inquiry Where to buy Suppliers range | GSK 962040 is a selective motilin receptor agonist with pEC50 value of 7.9. It is effective as a stimulant of human and rabbit gastrointestinal motility. lt represents a new opportunity as a treatment in diabetic gastroparesis. It is discovered as a therapeutic agent for conditions associated with delayed gastric emptying. It is highly selective against motilin receptor over the human ghrelin receptor and hERG. It also has no significant activity against other receptors including 5-HT, adrenergic, dopamine, histamine and adenosine receptors. It is found to enhance the EFS-induced cholinergic contraction and cause a small muscle contraction at high concentration in rabbit isolated gastric antrum. It also induces the contraction of human-isolated stomach preparations at 10μM. It had no significant activity at a range of other receptors (including ghrelin), ion channels and enzymes in vitro. It was preferred because its initial IC50 values at CYP3A4 were significantly higher than our preferred threshold of 10 μM. It induced phasic contractions, the duration of which was dose-related. It strongly facilitated cholinergic activity in the antrum, with lower activity in fundus and small intestine only. It was developed by glaxosmithkline and has been in Cilinic Phase 2. Uses: Gsk 962040 may be used as a treatment in diabetic gastroparesis. Synonyms: GSK-962040; GSK 962040; GSK962040; Camicinal;1-[4-(3-fluoroanilino)piperidin-1-yl]-2-[4-[[(3S)-3-methylpiperazin-1-yl]methyl]phenyl]ethanone. Grades: >98%. CAS No. 923565-21-3. Molecular formula: C25H33FN4O. Mole weight: 424.55. | |
Hyperforin DCHA Quick inquiry Where to buy Suppliers range | Key constituent of St. John's wort. Shows properties of potential pharmacological interest, including anti-bacterial, anti-malarial, anti-inflammatory, anti-cancer and anti-angiogenic effects. Anti-depressant and anxiolytic compound. Specific activator of TRPC6 channels. Inhibits the re-uptake of neurotransmitters in synapses (serotonin, norepinephrine, dopamine, GABA, glutamate). Activator of the pregnane X receptor (PXR). Regulates expression of the cytochrome P450 CYP3A4 and CYP2C9 and hepatic drugs metabolism. Potential anti-Alzheimer compound. Potent SIRT1 (sirtuin 1) and SIRT2 (sirtuin 2) inhibitor. Group: Biochemicals. Grades: Highly Purified. CAS No. 238074-03-8. Pack Sizes: 500ug, 1mg. Molecular Formula: C35H51O4 C12H24N. US Biological Life Sciences. | Worldwide |
Hyperforin DCHA (5-hydroxy-6R-methyl-1R, 3, 7S-tris(3-methyl-2-butenyl)-5S-(2-methyl-1-oxopropyl)-6R-(4-methyl-3-pentenyl)-bicyclo[3.3.1]non-3-ene-2,9-dione, DHCA) Quick inquiry Where to buy Suppliers range | Displays a variety of biological activities including anti-bacterial, anti-inflammatory, anticancer and anti-angiogenic effects. Also acts as an antidepressant and anxiolytic agent. Regulates expression of the cytochrome P450 CYP3A4 and CYP2C9 and hepatic drugs metabolism. Inhibits the re-uptake of neurotransmitters in synapses (serotonin, norepinephrine, dopamine, GABA, glutamate). Also acts as a potent SIRT1 and SIRT2 inhibitor. Group: Biochemicals. Grades: Highly Purified. CAS No. 238074-03-8. Pack Sizes: 500ug, 1mg. US Biological Life Sciences. | Worldwide |
Isoniazid Quick inquiry Where to buy Suppliers range | Antibiotic for treatment of Mycobacterium tuberculosis, inhibits mycolic acid biosynthesis. Metabolized by hepatic N-acetyltransferase (NAT) and cytochrome P450 2E1 (CYP2E1) to form hepatotoxins. Selectively induces expression of CYP2E1. Reversibly inhibits CYP2C19 and CYP3A4 activities, and mechanistically inactivates CYP1A2, CYP2A6, CYP2C19 and CYP3A4 at clinically relevant concentrations. Antibacterial (tuberculostatic). Group: Biochemicals. Alternative Names: 4-Pyridinecarboxylic Acid Hydrazide; Isonicotinic Acid Hydrazide; 4- (Hydrazinocarbonyl) pyridine; 4-Pyridinecarbonyl hydrazine; 4-Pyridinecarboxylic Hydrazide; 4-Pyridylcarbonyl hydrazide ; 5015 R.P.; Armazid; Armazide; Atcotibine;Isonizide; Isotebezid; Isozide; Robisellin; Sauterazid; Zinadon; Zonazide; Tubazid. Grades: Highly Purified. CAS No. 54-85-3. Pack Sizes: 1g. US Biological Life Sciences. | Worldwide |
Itraconazole Quick inquiry Where to buy Suppliers range | Itraconazole, a triazole antifungal agent, is a relatively potent inhibitor of CYP3A4. Uses: Antifungal agents; antiprotozoal agents. Synonyms: Itraconazole, R51211, R 51211, R-51211, Orungal, Oriconazole, Sporanox, Itraconazolum, Itraconazol, Itrizole. Grades: >98%. CAS No. 84625-61-6. Molecular formula: C35H38Cl2N8O4. Mole weight: 705.63. | |
K-11777 Quick inquiry Where to buy Suppliers range | K-11777 is a potent, irreversible cysteine protease inhibitor. Besides, K11777 is not only a substrate but also a mechanism-based inhibitor of CYP3A4. Synonyms: 4-methyl-N-((S)-1-oxo-3-phenyl-1-(((S,E)-5-phenyl-1-(phenylsulfonyl)pent-1-en-3-yl)amino)propan-2-yl)piperazine-1-carboxamide; APC-3316; APC3316; APC 3316; K-11777; K 11777; K11777; K 777; K-777; K777; CRA-3316; CRA3316; CRA 3316. Grades: >98%. CAS No. 233277-99-1. Molecular formula: C32H38N4O4S. Mole weight: 574.74. | |
Naloxegol Quick inquiry Where to buy Suppliers range | Naloxegol is a CYP3A4 enzyme inhibitor. It is also a peripherally-selective opioid antagonist. It is used as the treatment of opioid-induced constipation. lt is a pegylated (polyethylene glycol-modified) derivative of α-naloxol and can be used to reduce opioid-induced symptoms. lt binds to and blocks mu-opioid receptors in the peripheral nervous system. It would reverse the effects of opiate drugs of abuse if it entered the central nervous system. It was approved in 2014 in adult patients with chronic, non-cancer pain. lt was developed by AstraZeneca, licensed from Nektar Therapeutics. It was approved in 2014 in adult patients with chronic, non-cancer pain. It has been listed. Uses: Naloxegol is used as the treatment of opioid-induced constipation. lt can be used to reduce opioid-induced symptoms. Synonyms: Movantik;NKTR-118; NKTR 118; NKTR118; (4R, 4aS, 7S, 7aR, 12bS) -7- [2- [2- [2- [2- [2- [2- (2-methoxyethoxy) ethoxy] ethoxy] ethoxy] ethoxy] ethoxy] ethoxy] -3-prop-2-enyl-1, 2, 4, 5, 6, 7, 7a, 13-octahydro-4, 12-methanobenzofuro [3, 2-e] isoquinoline-4a, 9-diol. Grades: >98%. CAS No. 854601-70-0. Molecular formula: C34H53NO11. Mole weight: 651.78. | |
Naloxegol oxalate Quick inquiry Where to buy Suppliers range | Naloxegol oxalate is a CYP3A4 enzyme inhibitor, is a peripherally-selective opioid antagonist, for the treatment of opioid-induced constipation. Synonyms: Morphinan-3,14-diol, 4,5-epoxy-6-(3,6,9,12,15,18,21-heptaoxadocos-1-yloxy)-17-(2-propen-1-yl)-, (5α,6α)-, ethanedioate (1:1); AZ 13337019 oxalate; AZ13337019 oxalate; AZ-13337019 oxalate; Moventig; NKTR 118 oxalate; (4R,4aS,7S,7aR,12bS)-7-((2,5,8,11,14,17,20-heptaoxadocosan-22-yl)oxy)-3-allyl-1,2,3,4,5,6,7,7a-octahydro-4aH-4,12-methanobenzofuro[3,2-e]isoquinoline-4a,9-diol oxalate. Grades: >98%. CAS No. 1354744-91-4. Molecular formula: C36H55NO15. Mole weight: 741.82. | |
PDE10A Inhibitor, Cpd15 (Phosphodiesterase 10A Inhibitor, (6-chloro-3,8-dimethyl-1H-pyrazolo[3,4-b]quinolin-4-yl)(2-methylpyrimidin-5-yl)methanol) Quick inquiry Where to buy Suppliers range | A cell-permeable pyrazoloquinoline compound that acts as a potent phosphodiesterase 10A inhibitor (Ki≤5nM against human PDE10A), while exhibiting >500-fold selectivity over other human PDEs 1-11 and little activity against CYP3A4 (IC50 >20uM) or a panel of 23 kinases (IC50 >30uM). Reported to be orally available in monkey and rat species and be efficacious in reversing nMDAR antagonist (+)-MK-801-induced hyperactivity in a ratsl (MED = 10mg/kg p.o.) in vivo. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 5mg. Molecular Formula: C??H??ClN?O. US Biological Life Sciences. | Worldwide |
PF-4981517 Quick inquiry Where to buy Suppliers range | PF-4981517 (CYP3cide) is a potent, efficient, and specific time-dependent inactivator of human CYP3A4. Synonyms: CYP3cide, PF-04981517; PF 4981517; PF4981517. Grades: >98%. CAS No. 1390637-82-7. Molecular formula: C26H32N8. Mole weight: 456.59. | |
Reboxetine Quick inquiry Where to buy Suppliers range | Reboxetine, also called as Vestra, 2-((2-ethoxyphenoxy)benzyl)morpholine methanesulfonate, exists as two enantiomers, (R,R)-(-)- and (S,S)-(+)-reboxetine. Ti is a selective norepinephrine reuptake inhibitor used in the treatment of clinical depression, panic disorder and ADD/ADHD which has been approved for treatment of major depression. In vitro: it inhibits noradrenaline reuptake in vitro to a similar extent to the tricyclic antidepressant desmethylimipramine and does not inhibit the activity of the following isozymes of cytochrome P450: CYP1A2, CYP2C9, CYP2C19, and CYP2E1; In vivo: Reboxetine does not affect dopamine or serotonin reuptake and it has low in vivo and in vitro affinity for adrenergic, cholinergic, histaminergic, dopaminergic and serotonergic receptors.Besides, it inhibits both CYP2D6 and CYP3A4 with low binding affinities, but has shown no effect on the in vivo clearance of drugs metabolized by these enzymes. Inhibits (±)-epibatidine-induced Ca(2+) influx in human (h) muscle embryonic (hα1β1γδ) and adult (hα1β1εδ) AChRs in a non-competitive manner , with potencies IC50= 3.86±0.49 and 1.92±0.48 μM, respectively. Uses: A selective norepinephrine reuptake inhibitor used in the treatment of clinical depression, panic disorder and add/adhd, it has been approved for treatment of major depression. Synonyms: Norebox; 2-((2-ethoxyphenoxy)benzyl)morpholine methanesulfonate; Morpholine, 2-[(R)-(2-ethoxyphenoxy)phenylmethyl]-, (2R)-rel-; (R,R)-Reboxetine. Grades: ≥ 95.0%. CAS No. 98769-81-4. Molecular formula: C19H23NO3. Mole weight: 313.39. | |
Rolapitant HCl hydrate Quick inquiry Where to buy Suppliers range | Rolapitant, also known as SCH-619734, is a potent, highly selective, long-acting Neurokinin-1 (NK-1) receptor antagonist with potential antiemetic activity. Unlike other available NK-1 receptor antagonists, rolapitant is not an inhibitor of Cytochrome P450 enzyme CYP3A4 and has a long elimination half-life, allowing a single dose to prevent both acute and late-phase CINV during the first 120 hours post-chemotherapy. Synonyms: (5S, 8S) -8- ( ( (R) -1- (3, 5-bis (trifluoromethyl) phenyl) ethoxy) methyl) -8-phenyl-1, 7-diazaspiro[4. 5]decan-2-one hydrochloride.; SCH619734 SCH-619734; SCH 619734; Rolapitant HCl; Rolapitant hydrochloride, Rolapitant, brand name: Varubi. CAS No. 914462-92-3. Molecular formula: C25H26F6N2O2.ClH.H2O. Mole weight: 554.95. | |
SR 9186 Quick inquiry Where to buy Suppliers range | SR 9186 is an inhibitor of the cytochrome P450 isoform CYP3A4 with IC50 value of 0.011 μM. Synonyms: 1-[4-(4-Cyanophenyl)phenyl]-3-[4-(1H-imidazo[4,5-b]pyridin-7-yl)phenyl]urea. Grades: ≥95%. CAS No. 1361414-26-7. Molecular formula: C26H18N6O. Mole weight: 430.5. | |
TAK-700 Quick inquiry Where to buy Suppliers range | TAK-700 (Orteronel) is a potent and highly selective human 17,20-lyase inhibitor with IC50 of 38 nM, exhibits >1000-fold selectivity over other CYPs (e.g. 11-hydroxylase and CYP3A4). It completed two phase III clinical trials for metastatic, hormone-refractory prostate cancer but failed to extend overall survival rates, and development was voluntarily terminated as a result. Synonyms: TAK-700; TAK700; (S/R)-Orteronel; 6-(7-hydroxy-6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-7-yl)-N-methyl-2-naphthamide. Grades: >98%. CAS No. 426219-18-3. Molecular formula: C18H17N3O2. Mole weight: 307.35. | |
Tamoxifen Quick inquiry Where to buy Suppliers range | Tamoxifen is a selective estrogen response modifier (SERM), protein kinase C inhibitor and anti-angiogenetic factor. Tamoxifen is a prodrug that is metabolized to active metabolites 4-hydroxytamoxifen (4-OHT) and endoxifen by cytochrome P450 isoforms CYP2D6 and CYP3A4. In breast cancer, the gene repressor activity of tamoxifen against ERBB2 is dependent upon PAX2. Blocks estradiol-stimulated VEGF production in breast tumor cells. Protein kinase C inhibitor. Induces apoptosis in human malignant glioma cell lines. Tamoxifen and its metabolite 4-hydroxytamoxifen are selective estrogen response modifiers (SERMs) that act as estrogen antagonists in mammary gland. Blocks estradiol-stimulated VEGF production in breast tumor cells. Group: Biochemicals. Alternative Names: (Z)-2-[4-(1,2-Diphenyl-1-butenyl)phenoxy]-N,N-dimethylethanamine; ICI 47699; Mammaton; Novaldex; Tamoxifen; Z-Tamoxifen. Grades: Highly Purified. CAS No. 10540-29-1. Pack Sizes: 2.5g. US Biological Life Sciences. | Worldwide |
Tankyrase1/2 Inhibitor III (TNKS1/2 Inhibitor III, Wnt Pathway Inhibitor XIV, 3-(4-Methoxyphenyl)-5-((4-(4-methoxyphenyl)-5-methyl-4H-1,2,4-triazol-3-ylthio)methyl)-1,2,4-oxadiazole) Quick inquiry Where to buy Suppliers range | A cell-permeable triazolylthiomethyl-oxadiazole compound that binds TNKS1/PARP5a and TNKS2/PARP5b with high affinity (=79 and 28nM, respectively), and acts as a potent and reversible TNKS1/2 dual inhibitor (IC50=33nM TNKS2 in an auto-PARsylation assay). Shown to interact with the adenosine diphosphate linker portion of the NAD+ donor site, and display excellent selectivity over PARP1 and PARP2 activities (IC50>19uM); stabilize Axin2 levels (EC50=709nM in SW480 cells), and antagonize Wnt signaling (IC50=215nM in HEK293-SuperTopFlash assay). Exhibits minimal activity towards cytochrome P450 enzymes (IC50=21 and 5.7uM for CYP2C9 and CYP3A4) and hERG ion channel (IC50>30uM), and adequate microsomal stability. Group: Biochemicals. Grades: Highly Purified. CAS No. 865565-29-4. Pack Sizes: 10mg. US Biological Life Sciences. | Worldwide |