详情描述
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.
Product information
CAS Number: 1338259-05-4
Molecular Weight: 547.60
Formula: C33H29N3O5
Chemical Name: (S)-4'-((2,3-dimethyl-5-((1-(4-nitrophenyl)ethyl)carbamoyl)-1H-indol-1-yl)methyl)-[1,1'-biphenyl]-2-carboxylic acid
Smiles: C[C@H](NC(=O)C1=CC2=C(C=C1)N(CC1C=CC(=CC=1)C1=CC=CC=C1C(O)=O)C(C)=C2C)C1C=CC(=CC=1)[N+]([O-])=O
InChiKey: IIJDFXNUWZTHIM-NRFANRHFSA-N
InChi: InChI=1S/C33H29N3O5/c1-20-22(3)35(19-23-8-10-25(11-9-23)28-6-4-5-7-29(28)33(38)39)31-17-14-26(18-30(20)31)32(37)34-21(2)24-12-15-27(16-13-24)36(40)41/h4-18,21H,19H2,1-3H3,(H,34,37)(H,38,39)/t21-/m0/s1
Technical Data
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
In Vitro:
SR1664 was used at 2-10 µM final concentration in the in vitro assays.
In Vivo:
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.
References:
- 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.