BMS707035是一种 HIV-1 整合酶抑制剂，IC50为15 nM。

BMS-707035 is a specific HIV-I integrase (IN) inhibitor with IC50 of 15 nM. Phase 2.

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. [1] 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. [2]

729607-74-3

C17H19FN4O5S

410.42

N-[(4-氟苯基)甲基1,6-二氢-5-羟基-1-甲基-6-氧代-2-(四氢-1,1-二氧-2H-1,2-噻嗪-2-基)-4-嘧啶甲酰胺

H2O:<1 mgml
DMSO:36 mg/mL (87.7 mM)
Ethanol:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years