产品
编 号：F756079
分子式：C21H18BrN3O2S
分子量：456.36
分子式：C21H18BrN3O2S
分子量：456.36
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CAS No: 2803951-18-8
产品详情
生物活性：
URAT1 inhibitor 2 is an orally active and potent URAT1 and CYP isozyme inhibitor, with IC50 values of 1.36 μM, 16.97 μM, 5.22 μM for URAT1-mediated 14C-UA uptake, CYP1A2 and CYP2C9, respectively. URAT1 inhibitor 2 is a promising agent candidate in the study of hyperuricemia and gout.
体内研究：
URAT1 inhibitor 2 (Intravenous at 2 mg/kg or orally at 10 mg/kg) has excellent pharmacokinetic properties with the oral bioavailability of 59.3%.URAT1 inhibitor 2 (4, 2, 1, 0.5, and 0.25 mg/kg; Orally) shows orally active and outstanding SUA-lowering activity with a dose-dependent manner in acute hyperuricemia mice.URAT1 inhibitor 2 (1000 mg/kg, intragastric administration, once) shows favorable safety profiles and no obvious acute toxicity.Pharmacokinetic Parameters of URAT1 inhibitor 2 in male Sprague-Dawley rats.parameterunit p.o. i.v.
compoundmax (h)2323
AUC (0-t)ng/mL·h48754.616344.8
AUC (0-∞)ng/mL·h48781.516448.8
MRT (0-∞)h3.31.0
t1/2h2.21.8
Tmaxh0.3
Cmaxng/mL19185.0
CLmL/min/kg2.2
F%59.3
Animal Model:Male Sprague-Dawley rats (n=10)
Dosage:2 mg/kg (intravenous) or 10 mg/kg (oral administration)
Administration:Intravenous or oral administration
Result:Achieved excellent pharmacokinetic properties with the oral bioavailability of 59.3%.
Animal Model:Acute hyperuricemia mice
Dosage:4, 2, 1, 0.5, and 0.25 mg/kg
Administration:Orally, once
Result:Showed outstanding SUA-lowering activity.
Animal Model:Kunming mice
Dosage:1000 mg/kg
Administration:Itragastric administration, once
Result:Showed favorable safety profiles and no obvious acute toxicity.
体外研究：
URAT1 inhibitor 2 (compound 23) (0-50 μM, 3-20 min) inhibits URAT1-mediated 14C-UA uptake (IC50 = 1.36 μM) and CYP cells activity.
URAT1 inhibitor 2 is an orally active and potent URAT1 and CYP isozyme inhibitor, with IC50 values of 1.36 μM, 16.97 μM, 5.22 μM for URAT1-mediated 14C-UA uptake, CYP1A2 and CYP2C9, respectively. URAT1 inhibitor 2 is a promising agent candidate in the study of hyperuricemia and gout.
体内研究：
URAT1 inhibitor 2 (Intravenous at 2 mg/kg or orally at 10 mg/kg) has excellent pharmacokinetic properties with the oral bioavailability of 59.3%.URAT1 inhibitor 2 (4, 2, 1, 0.5, and 0.25 mg/kg; Orally) shows orally active and outstanding SUA-lowering activity with a dose-dependent manner in acute hyperuricemia mice.URAT1 inhibitor 2 (1000 mg/kg, intragastric administration, once) shows favorable safety profiles and no obvious acute toxicity.Pharmacokinetic Parameters of URAT1 inhibitor 2 in male Sprague-Dawley rats.parameterunit p.o. i.v.
compoundmax (h)2323
AUC (0-t)ng/mL·h48754.616344.8
AUC (0-∞)ng/mL·h48781.516448.8
MRT (0-∞)h3.31.0
t1/2h2.21.8
Tmaxh0.3
Cmaxng/mL19185.0
CLmL/min/kg2.2
F%59.3
Animal Model:Male Sprague-Dawley rats (n=10)
Dosage:2 mg/kg (intravenous) or 10 mg/kg (oral administration)
Administration:Intravenous or oral administration
Result:Achieved excellent pharmacokinetic properties with the oral bioavailability of 59.3%.
Animal Model:Acute hyperuricemia mice
Dosage:4, 2, 1, 0.5, and 0.25 mg/kg
Administration:Orally, once
Result:Showed outstanding SUA-lowering activity.
Animal Model:Kunming mice
Dosage:1000 mg/kg
Administration:Itragastric administration, once
Result:Showed favorable safety profiles and no obvious acute toxicity.
体外研究：
URAT1 inhibitor 2 (compound 23) (0-50 μM, 3-20 min) inhibits URAT1-mediated 14C-UA uptake (IC50 = 1.36 μM) and CYP cells activity.
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