Tenofovir,147127-20-6

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产品名称：Tenofovir

产品别名：替诺福韦

英文别名：GS 1278;PMPA;TDF

靶点：Reverse transcriptase

CAS：147127-20-6

纯度：0.99

外观：白色至类白色粉末

保存方法：Store at -20°C

描述：

Tenofovir能阻断HIV-1和HBV的逆转录酶，对HIV-1和HIV-2的IC50分别为0.5-2.2 uM和1.6-4.9 uM。

溶解性：DMSO : 4 mg/mL (13.92 mM), warmed
Water : 2 mg/mL (6.96 mM)

体外研究：

Tenofovir reduces the viral cytopathic effect of HIV-1(IIIB), HIV-2(ROD) and HIV(EHO) with EC50 of 1.15 μg/mL, 1.12 μg/mL and 1.05 μg/mL in MT-4 cells. Tenofovir also reduces the viral cytopathic effect of SIV(mac251) , SIV(B670) ,SHIV(89.6) and SHIV(RTSHIV). Tenofovir is uniquely active against multinucleoside-resistant HIV expressing the Q151M mutation, but shows reduced susceptibility to the T69S insertion mutations. Tenofovir inhibits hepatitis B virus (HBV) activity in HepG2 2.2.15, HepAD38 and HepAD79 cells. Tenofovir (4 μM) completely inhibits the growth of HIVIIIB in MT-2 cells. Tenofovir inhibits synthesis of negative strand strong-stop DNA with IC50 of 9 µM for wild-type RT, 6 µM for M184V RT and 50 µM for K65R RT.

体内研究：Tenofovir (30 mg/kg) completely prevents SIV infection in all macaques without toxicity. Tenofovir treatment reduces plasma viral RNA levels to undetectable, with parallel decreases in the infectivity of plasma and infectious cells in peripheral blood mononuclear cells and cerebrospinal fluid (CSF) and stabilization of CD4+ T-cell numbers. Tenofovir (30 mg/kg, s.c.) completely abrogates HIV infection via intravaginal exposure in pig-tailed macaques.

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