Darunavir ethanolate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的选择性 HIV-1 蛋白酶抑制剂，对实验室 HIV-1 菌株和主要临床分离株极其有效，IC50 为 3 nM，IC90 为 9 nM。

A potent, selective HIV-1 protease inhibitor that is extremely potent against laboratory HIV-1 strains and primary clinical isolates with IC50 of 3 nM, IC90 of 9 nM; blockes the infectivity and replication of HIV-1(NL4-3) variants with IC50 of 3-29 nM, also potent against multi-PI-resistant clinical HIV-1 variants isolated from patients; used to treat and prevent HIV/AIDS.HIV Infection Approved(In Vitro):Darunavir is a broad-spectrum potent inhibitor active against HIV-1 clinical isolates with minimal cytotoxicity. Darunavir forms hydrogen bonds with the conserved main-chain atoms of Asp29 and Asp30 of the protease. These interactions are proposed to be critical for the potency of this compound against HIV isolates that are resistant to multiple protease inhibitors. In an in vitro study in MT-2 cells, the potency of darunavir is greater than that of saquinavir, amprenavir, nelfinavir, indinavir, lopinavir and ritonavir. Darunavir is primarily metabolized by the hepatic cytochrome P450 (CYP) enzymes, primarily CYP3A. The ‘boosting’ dose of ritonavir acts an an inhibitor of CYP3A, thereby increasing darunavir bioavailability.(In Vivo):Darunavir is effective against wild-type and PI-resistant HIV, and has an oral bioavailability of 37%. It needs to be combined with ritonavir, which increases the bioavailability to 82%.

Darunavir is a broad-spectrum potent inhibitor active against HIV-1 clinical isolates with minimal cytotoxicity. Darunavir forms hydrogen bonds with the conserved main-chain atoms of Asp29 and Asp30 of the protease. These interactions are proposed to be critical for the potency of this compound against HIV isolates that are resistant to multiple protease inhibitors. In an in vitro study in MT-2 cells, the potency of darunavir is greater than that of saquinavir, amprenavir, nelfinavir, indinavir, lopinavir and ritonavir. Darunavir is primarily metabolized by the hepatic cytochrome P450 (CYP) enzymes, primarily CYP3A. The ‘boosting’ dose of ritonavir acts an an inhibitor of CYP3A, thereby increasing darunavir bioavailability.

Darunavir is effective against wild-type and PI-resistant HIV, and has an oral bioavailability of 37%. It needs to be combined with ritonavir, which increases the bioavailability to 82%.

TMC-114 | UIC-94017

Microbiology/Virology

HIV

WTHIV-1protease

Infection

HIV Infection

635728-49-3

593.732

C29H43N3O8S

>98% (HPLC)

10 mM in DMSO

CCO.CC(C)CN(C[C@H]([C@H](CC1=CC=CC=C1)NC(=O)O[C@H]2CO[C@@H]3[C@H]2CCO3)O)S(=O)(=O)C4=CC=C(C=C4)N

Carbamic acid, N-[(1S,2R)-3-[[(4-aminophenyl)sulfonyl](2-methylpropyl)amino]-2-hydroxy-1-(phenylmethyl)propyl]-, (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl ester, compd. with ethanol (1:1)

(-20℃)

With Ice Pack

≥ 2 years