产品
编 号：F747194
分子式：C34H43FN2O4
分子量：562.71
分子式：C34H43FN2O4
分子量：562.71
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CAS No: 1803444-21-4
产品详情
生物活性：
GSK3739936 (BMS-986180) is a potent HIV-1 allosteric integrase inhibitor with an IC50 value of 11.1 nM and an EC50 value of 1.7 nM. GSK3739936 is also a weak CYP inhibitor (IC50>24.3 μM). GSK3739936 shows favorable pharmacokinetic property in preclinical species with rapid absorption, low to moderate clearance and excellent oral bioavailability.
体内研究：
GSK3739936 exhibits favorable pharmacokinetic property with rapid absorption, low to moderate clearance and excellent oral bioavailability.Pharmacokinetic Parameters of GSK3739936 in Preclinical Species.Male CD-1 mice Male Sprague-Dawley rats Cynomolgus monkey Male beagle dogs
IV dose (mg/kg)1111
CL (mL/min/kg)5.45.514.52.9
t1/2 (h)6.34.32.45.1
Vss (L/kg)2.41.81.50.7
PO dose (mg/kg)5522
Cmax (nM)236127625252963
tmax (h)52.722
AUC (nM·h)2451614022223118471
F (%)89525475
Animal Model:Male CD-1 mice, male Sprague-Dawley rats, cynomolgus monkey and male beagle dogs
Dosage:1 mg/kg for IV; 5 or 2 mg/kg for PO
Administration:PO or IV; single dosage
Result:Exhibited a low clearance in the mouse, rat, and dog with moderate to long elimination half-lives, while displays moderate clearance and a short elimination half-life in the cynomolgus monkey.The absolute oral bioavailability ranged between 52 and 89%.The tmax value of 2-5 h suggesting rapid absorption in all four species.
体外研究：
GSK3739936 is not cytotoxic to MT-2 cells, exhibiting CC50 values of >20 μM.
GSK3739936 (BMS-986180) is a potent HIV-1 allosteric integrase inhibitor with an IC50 value of 11.1 nM and an EC50 value of 1.7 nM. GSK3739936 is also a weak CYP inhibitor (IC50>24.3 μM). GSK3739936 shows favorable pharmacokinetic property in preclinical species with rapid absorption, low to moderate clearance and excellent oral bioavailability.
体内研究：
GSK3739936 exhibits favorable pharmacokinetic property with rapid absorption, low to moderate clearance and excellent oral bioavailability.Pharmacokinetic Parameters of GSK3739936 in Preclinical Species.Male CD-1 mice Male Sprague-Dawley rats Cynomolgus monkey Male beagle dogs
IV dose (mg/kg)1111
CL (mL/min/kg)5.45.514.52.9
t1/2 (h)6.34.32.45.1
Vss (L/kg)2.41.81.50.7
PO dose (mg/kg)5522
Cmax (nM)236127625252963
tmax (h)52.722
AUC (nM·h)2451614022223118471
F (%)89525475
Animal Model:Male CD-1 mice, male Sprague-Dawley rats, cynomolgus monkey and male beagle dogs
Dosage:1 mg/kg for IV; 5 or 2 mg/kg for PO
Administration:PO or IV; single dosage
Result:Exhibited a low clearance in the mouse, rat, and dog with moderate to long elimination half-lives, while displays moderate clearance and a short elimination half-life in the cynomolgus monkey.The absolute oral bioavailability ranged between 52 and 89%.The tmax value of 2-5 h suggesting rapid absorption in all four species.
体外研究：
GSK3739936 is not cytotoxic to MT-2 cells, exhibiting CC50 values of >20 μM.
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