Lersivirine(UK 453061)

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

Lersivirine（UK 453061）是第二代非核苷逆转录酶抑制剂（NNRTI），正在开发用于治疗 HIV 感染。

Lersivirine(UK 453061) is a second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) under development for HIV infection therapy.?(In Vitro):Lersivirine demonstrates excellent activity against large panels of wild type and drug-resistant HIV consistent with the encouraging profile demonstrated against the isolated RT enzymes.(In Vivo):Lersivirine (oral gavage; 0, 150, 350, and 500 mg/kg; once daily; gestation days 6 to 17, followed by cesarean section on gestation day 18. ) allows induction of hepatic metabolizing enzymes at the first 2 days at 250 mg/kg, after which the dose is increased to 500 mg/kg/day in Mated Crl:CD1(ICR) mice. Lersivirine leads to skeletal variations which related to delayed development and decreased fetal ossifications.

Lersivirine demonstrates excellent activity against large panels of wild type and drug-resistant HIV consistent with the encouraging profile demonstrated against the isolated RT enzymes.

Lersivirine (oral gavage; 0, 150, 350, and 500 mg/kg; once daily; gestation days 6 to 17, followed by cesarean section on gestation day 18. ) allows induction of hepatic metabolizing enzymes at the first 2 days at 250 mg/kg, after which the dose is increased to 500 mg/kg/day in Mated Crl:CD1(ICR) mice. Lersivirine leads to skeletal variations which related to delayed development and decreased fetal ossifications.

Lersivirine | UK-453061

Microbiology/Virology

HIV

HIV

Inflammation/Immunology

HIV-1

473921-12-9

310.35

C17H18N4O2

>98% (HPLC)

DMSO:50 mg/mL (161.11 mM; Need ultrasonic)

CCc1nn(CCO)c(CC)c1Oc1cc(C#N)cc(C#N)c1

5-((35-diethyl-1-(2-hydroxyethyl)-1H-pyrazol-4-yl)oxy)isophthalonitrile

(-20℃)

With Ice Pack

≥ 2 years