SR1664 is a potent and selective PPARγ inhibitor with potential antidiabetic activity. SR1664 binds to PPARγ and potently inhibits Cdk5-mediated PPARγ phosphorylation (IC50 = 80 nM; Ki = 28.67 nM) without exhibiting PPARγ agonist activity.
CAS Number: 1338259-05-4
Molecular Weight: 547.60
Chemical Name: (S)-4'-((2,3-dimethyl-5-((1-(4-nitrophenyl)ethyl)carbamoyl)-1H-indol-1-yl)methyl)-[1,1'-biphenyl]-2-carboxylic acid
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 25 mM
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: ≥360 days 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
SR1664 was used at 2-10 µM final concentration in the in vitro assays.
SR1664 was injected intraperitoneally at 40 mg/kg twice per day for 5 days and showed good efficacy in high-fat diet (HFD) and db/db mouse models.
- Choi JH, et al. Antidiabetic actions of a non-agonist PPARγ ligand blocking Cdk5-mediated phosphorylation. (2011) Nature. 477(7365):477-81.
- Norris AW, at al. A second chance for a PPARγ targeted therapy? (2012) Circ Res. 110(1):8-11.
Products are for research use only. Not for human use.
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