
货号:M1361
储存条件:粉末-20°C可保存3年;液体-80°C可保存12月。
产品描述
Maraviroc is a reversible antagonist of C-C chemokine receptor type 5 (CCR5), which inhibits the interaction between CCR5 with the envelop glycoprotein gp120 of human immunodeficiency virus-1 (HIV-1), thus blocking HIV-1 entry into cells. The overall in vitro IC50 of maraviroc ranges from 0.1 to 4.5 nM. Incubation with maraviroc-contained medium at the concentration of 0.1 μM for 48 hours induced CCR5 surface expression on activated T cells. Moreover, 24-hour treatment of 1 μM to 100 μM maraviroc inhibited T cell migration induced by various chemokines. T cell proliferation was also shown to be inhibited after 72-hour incubation with 100 μM maraviroc. A study in female RAG-hu mice showed that 5 mM maraviroc, which was applied into the vaginal vault of mice one hour before viral challenge, fully prevented HIV-1 vaginal transmission. Mice with diet-induced hepatocellular carcinoma showed reduced liver fibrosis, lower levels of liver injury markers, and decreased proliferation index with the treatment of 300 mg/L maraviroc added in drinking water for 16 weeks. A phase 2 trial reported that 300 mg/kg maraviroc twice daily decreased the viral loads by 1.6log10 copies/mL in asymptomatic HIV-1-infected patients.
产品信息
CAS号 | 376348-65-1 | |
分子式 | C29H41F2N5O | |
分子量 | 513.67 | |
溶解度
| DMSO | 360.0 mg/mL (700.8 mM) warming |
Water | insoluble | |