Ritonavir是一种HIV蛋白酶抑制剂，用于治疗HIV感染和AIDS。 产品介绍： Ritonavir (ABT 538) 是用于研究 HIV 感染和 AIDS 的 HIV 蛋白酶的抑制剂。Ritonavir 也是 SARS-CoV 3CLpro 的抑制剂，IC50 为 1.61 μM。 Information Ritonavir (ABT-538, A 84538, RTV, Norvir, Norvir Softgel) is aCytochrome P450 3AandProteaseInhibitor; Also inhibitsCytochrome P450 2D6,P-Glycoproteinand inducesCytochrome P450 2C19,Cytochrome P450 1A2,Cytochrome P450 2C9,Cytochrome P450 2B6andUDP Glucuron In vitro Ritonavir is a very potent inhibitor of CYP3A4 mediated testosterone 6β-hydroxylation with mean Ki of 19 nM and also inhibits tolbutamide hydroxylation with IC50 of 4.2 μM. Ritonavir is found to be a potent inhibitor of CYP3A-mediated biotransformations (nifedipine oxidation with IC50 of 0.07 mM, 17alpha-ethynylestradiol 2-hydroxylation with IC50 of 2 mM; terfenadine hydroxylation with IC50 of 0.14 mM). Ritonavir is also found to be an inhibitor of the reactions mediated by CYP2D6 (IC50 = 2.5 mM) and CYP2C9/10 (IC50 = 8.0 mM). Ritonavir results in an increase in cell viability in uninfected human PBMC cultures. Ritonavir markedly decreases the susceptibility of PBMCs to apoptosis correlated with lower levels of caspase-1 expression, decreases in annexin V staining, and reduces caspase-3 activity in uninfected human PBMC cultures. Ritonavir inhibits induction of tumor necrosis factor (TNF) production by PBMCs and monocytes in a time- and dose-dependent manner at nontoxic concentrations. Ritonavir inhibits p-glycoprotein-mediated extrusion of saquinavir with an IC50 of 0.2 μM, indicating a high affinity of ritonavir for p-glycoprotein. Ritonavir inhibits human liver microsomal metabolism of ABT-378 potently with Ki of 13 nM. Ritonavir combined with ABT-378 (at 3:1 and 29:1 ratios) inhibits CYP3A (IC50 = 1.1 and 4.6 μM), albeit less potently than Ritonavir (IC50 = 0.14 μM). In vivo Cell Data cell lines： Concentrations： Incubation Time： Powder Purity:≥98%
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Ritonavir (ABT-538)
CAS number：155213-67-5(DMSO) molecular formula：C37H48N6O5S2
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| Chinese alias | 利托那韦（ABT-538） | ||
| English alias | A 84538, RTV, Norvir, Norvir Softgel | (3S,4S,6S,9S)-4-hydroxy-12-methyl-9-(1-methylethyl)-13-[2-(1-methylethyl)-4-thiazolyl]-8,11-dioxo-3,6-bis(phenylmethyl)-2,7,10,12-Tetraazatridecanoic acid 5-thiazolylmethyl ester | ||
| CAS number | 155213-67-5(DMSO) | molecular formula | C37H48N6O5S2 |
| molecular weight | 720.94 g/mol | Exact mass | - |
| PSA | - | logp | - |
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