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Ritonavir

CAS No. : 155213-67-5

MCE 国际站：Ritonavir

产品活性：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 3CL^pro 的抑制剂，IC₅₀ 为 1.61 μM。

研究领域：Anti-infection  |  Metabolic Enzyme/Protease  |  Apoptosis

作用靶点：HIV Protease  |  HIV  |  SARS-CoV  |  Apoptosis

In Vitro: Ritonavir (ABT 538) is an inhibitor of CYP3A4 mediated testosterone 6β-hydroxylation with mean K_i of 19 nM and also inhibits tolbutamide hydroxylation with IC₅₀ of 4.2 μM.
Ritonavir (ABT 538) 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 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 K_i 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).

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