DS-6930_product_DataBase

Bioactivity	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[1].
Invitro	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) [1].DS-6930 (10-100 µM) exhibits lower cell toxicity at 100 µM[1].
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[1].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[1].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[1].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[1].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[1]. Animal Model:
Name	DS-6930
CAS	1242328-82-0
Formula	C23H21N3O4
Molar Mass	403.43
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Shinozuka T, et, al. Discovery of DS-6930, a potent selective PPARγ modulator. Part II: Lead optimization. Bioorg Med Chem. 2018 Oct 1;26(18):5099-5117.

PeptideDB

DS-6930

CAS: 1242328-82-0 F: C23H21N3O4 W: 403.43