BMS-707035是一种特异性的HIV-I integrase (IN)（整合酶）抑制剂，IC50为15 nM。BMS-707035是与Raltegravir相似的嘧啶酰胺, 是第一个应用到临床的整合酶抑制剂。BMS-707035 是有效的，特定 HIV的可逆抑制剂，抑制HIV整合酶链转移活性，IC50为15 nM。然而, 一些整合酶突变型, 包括 V75I, Q148R, V151I, 和G163R 对HIV 整合酶抑制剂具有抗性。

98%

Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.

DMSO ：36 mg/mL (87.7 mM)

HIV-I integrase

BMS-707035 is a pyrimidine carboxamide similar to Raltegravir, the first integrase inhibitor licensed for clinical use. BMS-707035 is a potent, specific, and reversible HIV-I integrase (IN) inhibitor that blocks HIV IN strand transfer activity with IC50 of 15 nM. However, several IN mutations, including V75I, Q148R, V151I, and G163R are found to confer resistance to HIV IN inhibitors. The binding of BMS-707035 and target DNA to IN are mutually exclusive events, as revealed by the fact that the inhibition of strand transfer catalysis by BMS-707035 is overcome by increasing amount of target DNA. The binding affinity of BMS-707035 to IN is also affected by the four terminal bases at the 5′ end of the pre-processed U5 long terminal repeat (LTR). Gln148 of IN is crucial for the binding of BMS-707035 to IN. The 3′ terminus of the viral LTR, on the other hand, retards the rate of BMS-707035 association with IN, by regulating the kinetics of binding and dissociation.

Anti-infectives: clinical progress of HIV-1 integrase inhibitors.
Al-Mawsawiet al. Expert Opin Emerg Drugs. 2008 Jun;13(2):213-25. PMID: 18537517.
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