Cat. No. Name Size Price Add Cart
KI1290Ritonavir10 mg$144
Ritonavir50 mg$592
Ritonavir100 mg$912

Chemical Characteristic

Product NameRitonavir
SynonymsNorvir
CAS No.155213-67-5
Molecular Weight 720.95
FormulaC37H48N6O5S2
Chemical Name1,3-Thiazol-5-ylmethyl N-[(2S,3S,5R)-3-hydroxy-5-[[(2S)-3-methyl-2-[[methyl-[(2-propan-2-yl-1,3-thiazol-4-yl)methyl]carbamoyl]amino]butanoyl]amino]-1,6-diphenyl-hexan-2-yl]carbamate
SmilesC(=O)(NC(Cc1ccccc1)[C@@H](C[C@@H](Cc1ccccc1)NC(=O)[C@H](C(C)C)NC(=O)N(Cc1nc(sc1)C(C)C)C)O)OCc1scnc1
Chemical Structure

Biological activities

Ritonavir is a HIV protease inhibitor used as an antiretroviral drug. Ritonavir is used to treat HIV infection and AIDS. The IC50 of ritonavir is 0.14 µM.[1]Ritonavir is a very potent inhibitor of CYP3A4 mediated testosterone 6β-hydroxylation with an 19 nM. Ritonaviralso preventstolbutamide hydroxylation with an IC50 of 4.2µM.[2]Ritonavir inhibits p-glycoprotein-mediated extrusion of saquinavir with an IC50 of 0.2 µM.[3]Ritonavir slows the proliferation of human myeloid leukemia cells and enhances their differentiation in the presence of all??rans-retinoic acid. Ritonavir inhibits the growth of DU145 and PC-3 androgen-independent prostate cancer cells. Ritonavir enhances the antiproliferative and proapoptotic effects of docetaxel in the hormonally independent DU145 prostate cancer cells in vitro. Ritonavir inhibits DNA binding activity of nuclear factor κB (NFκB) in DU145 cells.Combination treatment of docetaxel and ritonavir dramatically suppresses the growth of DU145 cells present as tumor xenografts in BNX nude mice.Ritonavir also preventsNFκB DNA binding activity in DU145 xenografts.[4]Coadministration of other protease inhibitors (such as indinavir, nelfinavir) with ritonavir in rats and dogs generates elevated and sustained plasma drug levels 8 to 12 hours after a single dose.[5]

Protocols

In vivo: Ritonavir is dissolved in 0.1% DMSO.[4]

References

[1]von Moltke LL, et al.Potent mechanism-based inhibition of human CYP3A in vitro by amprenavir and ritonavir: comparison with ketoconazole.Eur J ClinPharmacol. 2000, 56(3):259-261.
[2]Eagling VA, et al. Differential inhibition of cytochrome P450 isoforms by the protease inhibitors, ritonavir, saquinavir and indinavir.Br J ClinPharmacol. 1997, 44(2): 190-194.
[3]Drewe J, et al.HIV protease inhibitor ritonavir: a more potent inhibitor of P-glycoprotein than the cyclosporine analog SDZ PSC 833.BiochemPharmacol. 1999, 57(10):1147-1152.
[4]Ikezoe T, et al. HIV-1 protease inhibitor, ritonavir: a potent inhibitor of CYP3A4, enhanced the anticancer effects of docetaxel in androgen-independent prostate cancer cells in vitro and in vivo.Cancer Res. 2004, 64(20):7426-7431.
[5]Kempf DJ, et al.Pharmacokinetic enhancement of inhibitors of the human immunodeficiency virus protease by coadministration with ritonavir.Antimicrob Agents Chemother. 1997, 41(3):654-660.

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