Description
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.
Product information
CAS Number: 1242328-82-0
Molecular Weight: 403.43
Formula: C23H21N3O4
Chemical Name: 3-({6-[(3,5-dimethylpyridin-2-yl)oxy]-1-methyl-1H-1,3-benzodiazol-2-yl}methoxy)benzoic acid
Smiles: CC1=CN=C(OC2C=C3C(=CC=2)N=C(COC2=CC(=CC=C2)C(O)=O)N3C)C(C)=C1
InChiKey: GEGLFSVXCSGSOB-UHFFFAOYSA-N
InChi: InChI=1S/C23H21N3O4/c1-14-9-15(2)22(24-12-14)30-18-7-8-19-20(11-18)26(3)21(25-19)13-29-17-6-4-5-16(10-17)23(27)28/h4-12H,13H2,1-3H3,(H,27,28)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
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.
In Vivo:
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.
Products are for research use only. Not for human use.
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