DS-6930

Research use only, not for human use.

DS-6930 (DS 6930, DS6930) is a novel potent, selective PPARγ agonist with EC50 of 41 nM.

DS-6930 (DS 6930, DS6930) is a novel potent, selective PPARγ agonist with EC50 of 41 nM, Emax-68%; significantly recruits several cofactors, such as RIP140 and PGC1, in cofactor recruitment assays; demonstrateshigh PPARγ agonist potency with robust plasma glucose reduction, maintains diminished PPARγ-related adverse effects upon toxicological evaluation in vivo, and demonstrated no hepatotoxicity.Diabetes Discontinued.

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 (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.

DS 6930 | DS6930

Metabolic Enzyme/Protease

PPAR

PPAR

Metabolic Disease

Diabetes

1242328-82-0

403.438

C23H21N3O4

>98% (HPLC)

——

CC1=CC(=C(N=C1)OC2=CC3=C(C=C2)N=C(N3C)COC4=CC=CC(=C4)C(=O)[O-])C.CC1=CC(=C(N=C1)OC2=CC3=C(C=C2)N=C(N3C)COC4=CC=CC(=C4)C(=O)[O-])C.[Ca+2]

3-((6-((3,5-dimethylpyridin-2-yl)oxy)-1-methyl-1H-benzo[d]imidazol-2-yl)methoxy)benzoic acid calcium salt

(-20℃)

With Ice Pack

≥ 2 years