Ritonavir

Ritonavir is an HIV protease inhibitor. It inhibits recombinant HIV-1 protease by 79% when used at a concentration of 0.5 nM. It inhibits HIV-13B-induced cell death in MT-4 human T cell leukemia cells (EC50 = 25 nM) as well as cell death induced by HIV-1LAI, HIV-2ROD, and HIV-2EHO in human MT-2 cells (IC50s = 0.045, 0.13, and 0.24 µM, respectively). Ritonavir also inhibits the cytochrome P450 (CYP) isoform CYP3A (IC50 = 0.14 µM). It inhibits CYP-mediated oxidative metabolism of the HIV protease inhibitors saquinavir (Cay-9001893), indinavir (Cay-15150), nelfinavir (Cay-15144), and amprenavir (Cay-15369) in rat and human liver microsomes in a concentration-dependent manner. Ritonavir (10 mg/kg) also prevents decreases in plasma levels of these four compounds in rats. Formulations containing ritonavir have been used in the treatment of HIV-1 infection.Formal Name: (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. Synonyms: A-84538, ABT-538, NSC 693184, RTV. Molecular Formula: C37H48N6O5S2. Formula Weight: 720.9. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 15 mg/ml, DMSO: 15 mg/ml, DMSO:PBS(pH 7.2) (1:2): 0.1 mg/ml, Ethanol: 5 mg/ml. lambdamax: 238 nm. SMILES: O[C@H]([C@@H](NC(OCC1=CN=CS1)=O)CC2=CC=CC=C2)C[C@@H](NC([C@H](C(C)C)NC(N(C)CC3=CSC(C(C)C)=N3)=O)=O)CC4=CC=CC=C4. InChi Code: InChI=1S/C37H48N6O5S2/c1-24(2)33(42-36(46)43(5)20-29-22-49-35(40-29)25(3)4)34(45)39-28(16-26-12-8-6-9-13-26)18-32(44)31(17-27-14-10-7-11-15-27)41-37(47)48-21-30-19-38-23-50-30/h6-15,19,22-25,28,31-33,44H,16-18,20-21H2,1-5H3,(H,39,45)(H,41,47)(H,42,46. InChi Key: NCDNCNXCDXHOMX-XGKFQTDJSA-N.