DS-6930 

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].

DS-6930 exhibits high potency in vitro with an intermediate PPARγ agonist activity (EC₅₀=41 nM, E_max=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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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 C_max=0.0792 µg/mL, T_max=1.8 h, and AUC_0-24h=0.861 h•µg/mL following oral (0.3 mg/kg) administration on day 22 in rats^[1].
DS-6930 exhibits C_max=2.25 µg/mL, T_max=5.0 h, T_1/2=13.5 h, and AUC_last=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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

403.43

C₂₃H₂₁N₃O₄

1242328-82-0

O=C(O)C1=CC=CC(OCC2=NC3=CC=C(OC4=NC=C(C)C=C4C)C=C3N2C)=C1

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]