产品
编 号:F440208
分子式:C17H19FN4O5S
分子量:410.42
产品类型
结构图
CAS No: 729607-74-3
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产品详情
生物活性:
BMS-707035 is a potent orally active HIV-1 integrase strand transfer inhibitor (INSTI). BMS-707035 has enzyme inhibitory with an IC50 value of 3 nM. BMS-707035 also has weak CYP inhibiton and antiviral activity. BMS-707035 can be used for the research of human immunodeficiency virus-1 (HIV-1).
体内研究:
BMS-707035 has a low clearance effect in the rat, dog and monkey with moderate to long elimination half-lives in all species.Pharmacokinetic Parameters of BMS-707035 in rat, dog and monkey (IV). RatMonkeyDog
IV dose (mg/kg)0.8711
CL (ml/min/kg) 9.76.82.0
T1/2(h)4.06.56.0
Vss(L/kg)0.860.870.45
PO dose (mg/kg)4.455.2
Cmax(μM)4.51 6.12 72.8
tmax(h)0.250.250.25
AUC (μM*h) 19.1 19.2162
F (%)8656129
体外研究:
BMS-707035 has antiviral activity with EC50 values of 2 nM and 17 nM in the presence of 10% FBS and 15 mg/mL human serum albumin, respectively.BMS-707035 has high plasma protein binding and not overtly cytotoxicy to several cell lines, with CC50 value of ≥45 μM.BMS-707035 has a relatively weak CYP inhibiton with IC50 value of ≥40 μM.