HIV protease inhibitor
CAS：155213-67-5
分子式：C37H48N6O5S2
分子量：720.9
纯度：98%
存储：Store at -20°C

Background:

Ritonavir, previously known as ABT-538, is a potent inhibitor of human immunodeficiency virus type 1 (HIV-1) protease that exhibits potent in vitro inhibition against HIV-1 strain as well as HIV-2 strain with 50% effective concentration EC₅₀values of 0.022 μM and 0.16 μM respectively. Ritonavir binds to the HIV-1 protease inactivating its function to cleave the Gag and Gag-Pol polyproteins into the core proteins and viral enzymes, which results in the formation of noninfectious viral particles. X-ray crystallographic analysis reveals a hydrophobic cluster between the isopropyl substituent on the P3 thiazolyl group of ritonavir and the side chains of Pro-81 and Val-82 of HIV-1 protease within the complex of ritonavir/HIV-1 protease.

Reference

[1].Kempf DJ, Marsh KC, Denissen JF, McDonald E, Vasavanonda S, Flentge CA, Green BE, Fino L, Park CH, Kong XP, et al. ABT-538 is a potent inhibitor of human immunodeficiency virus protease and has high oral bioavailability in humans. Proc Natl Acad Sci U S A. 1995 Mar 28;92(7):2484-8.
[2].Markowitz M, Saag M, Powderly WG, Hurley AM, Hsu A, Valdes JM, Henry D, Sattler F, La Marca A, Leonard JM, et al. A preliminary study of ritonavir, an inhibitor of HIV-1 protease, to treat HIV-1 infection. N Engl J Med. 1995 Dec 7;333(23):1534-9.