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).
性状
Solid
体外研究(In Vitro)
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.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
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).
Rat
Monkey
Dog
IV dose (mg/kg)
0.87
1
1
CL (ml/min/kg)
9.7
6.8
2.0
T1/2(h)
4.0
6.5
6.0
Vss(L/kg)
0.86
0.87
0.45
PO dose (mg/kg)
4.4
5
5.2
Cmax(μM)
4.51
6.12
72.8
tmax(h)
0.25
0.25
0.25
AUC (μM*h)
19.1
19.2
162
F (%)
86
56
129
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.