产品
编 号：F673488
分子式：C23H21N3O4
分子量：403.43
分子式：C23H21N3O4
分子量：403.43
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CAS No: 1242328-82-0
产品详情
生物活性：
DS-6930 is a potent and selective agonist of PPARγ, with an EC50 of 41 nM. DS-6930 could robust reduce plasma glucose (PG), and with fewer PPARγ-related adverse effects than Rosiglitazone. DS-6930 can be used for the research of diabetes.
体内研究：
DS-6930 (0.1-3 mg/kg; p.o. for 3 weeks) decreases plasma glucose (PG) levels in a dose-dependent manner in rats.DS-6930 (100-1000 mg/kg; p.o.for 4 weeks) does not affect any liver enzyme activities and has no remarkable change in relative heart weigh in F344 rats.DS-6930 exhibits Cmax=0.0792 μg/mL, Tmax=1.8 h, and AUC0-24h=0.861 h?μg/mL following oral (0.3 mg/kg) administration on day 22 in rats.DS-6930 exhibits Cmax=2.25 μg/mL, Tmax=5.0 h, T1/2=13.5 h, and AUClast=23.5 h?μg/mL following oral (3 mg/kg) administration in cynomolgus monkeys.DS-6930 exhibits excellent bioavailability (F=89%), total body clearance (CL=2.06 mL/min/kg), and distribution volume at steady state (Vss=0.36 L/kg) following intravenous (1 mg/kg) administration in cynomolgus monkeys.Animal Model:Male ZDF rats
Dosage:0.1, 0.3, 1, 3 mg/kg
Administration:P.o. daily for 3 weeks
Result:47% PG reduction at dose of 0.3 mg/kg vs vehicle control.
Animal Model:Male ZDF rats
Dosage:0.3 mg/kg (Pharmacokinetic Analysis)
Administration:P.o. daily for 22 days
Result:Cmax=0.0792 μg/mL; Tmax=1.8 h; AUC0-24h=0.861 h?μg/mL.
体外研究：
DS-6930 exhibits high potency in vitro with an intermediate PPARγ agonist activity (EC50=41 nM, Emax=68%), and possesses high PPARα or PPARδ selectivity (13% PPARα activation at 10 μM and no PPARδ activation at 10 μM) .DS-6930 (10-100 μM) exhibits lower cell toxicity at 100 μM.
DS-6930 is a potent and selective agonist of PPARγ, with an EC50 of 41 nM. DS-6930 could robust reduce plasma glucose (PG), and with fewer PPARγ-related adverse effects than Rosiglitazone. DS-6930 can be used for the research of diabetes.
体内研究：
DS-6930 (0.1-3 mg/kg; p.o. for 3 weeks) decreases plasma glucose (PG) levels in a dose-dependent manner in rats.DS-6930 (100-1000 mg/kg; p.o.for 4 weeks) does not affect any liver enzyme activities and has no remarkable change in relative heart weigh in F344 rats.DS-6930 exhibits Cmax=0.0792 μg/mL, Tmax=1.8 h, and AUC0-24h=0.861 h?μg/mL following oral (0.3 mg/kg) administration on day 22 in rats.DS-6930 exhibits Cmax=2.25 μg/mL, Tmax=5.0 h, T1/2=13.5 h, and AUClast=23.5 h?μg/mL following oral (3 mg/kg) administration in cynomolgus monkeys.DS-6930 exhibits excellent bioavailability (F=89%), total body clearance (CL=2.06 mL/min/kg), and distribution volume at steady state (Vss=0.36 L/kg) following intravenous (1 mg/kg) administration in cynomolgus monkeys.Animal Model:Male ZDF rats
Dosage:0.1, 0.3, 1, 3 mg/kg
Administration:P.o. daily for 3 weeks
Result:47% PG reduction at dose of 0.3 mg/kg vs vehicle control.
Animal Model:Male ZDF rats
Dosage:0.3 mg/kg (Pharmacokinetic Analysis)
Administration:P.o. daily for 22 days
Result:Cmax=0.0792 μg/mL; Tmax=1.8 h; AUC0-24h=0.861 h?μg/mL.
体外研究：
DS-6930 exhibits high potency in vitro with an intermediate PPARγ agonist activity (EC50=41 nM, Emax=68%), and possesses high PPARα or PPARδ selectivity (13% PPARα activation at 10 μM and no PPARδ activation at 10 μM) .DS-6930 (10-100 μM) exhibits lower cell toxicity at 100 μM.
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