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BMS-707035 结构式

BMS-707035

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货号 :BCP02412CAS号 :729607-74-3纯度:98%
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  • 基本信息与产品描述
CAS号 729607-74-3 货号 BCP02412
中文名 BMS-707035
英文名 BMS-707035
中文别名
英文别名 BMS707035;BMS 707035;
SMILES
化学名称
分子式 C17H19FN4O5S 分子量 410.42
纯度 98% 配送 惯例下常温包邮
产品描述 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. [1] 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.
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