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BMS-707035
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BMS-707035图片
CAS NO:729607-74-3
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
50 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
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
产品介绍
BMS707035是一种 HIV-1 整合酶抑制剂,IC50为15 nM。

产品描述

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

体外活性

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. [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]

Cas No.

729607-74-3

分子式

C17H19FN4O5S

分子量

410.42

别名

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

储存和溶解度

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