BMS-707035
| 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; | ||
| 分子式 | C17H19FN4O5S | 分子量 | 410.42 |
| 生物活性 | 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. | ||
| 信号通路 | Protease/Metabolic Enzyme Microbiology/Virology | ||
| 靶 点 | Integrase HIV | ||
结构式
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