For research use only. Not for therapeutic Use.
SR1664 is a PPARγ antagonist. SR1664 binds to PPARγ and potently inhibits Cdk5-mediated PPARγ phosphorylation (IC50=80 nM; Ki= 28.67 nM)[1][2].
SR1664 (1uM; HEK293T cells) pharmacological effect on PPARγ activity is altered by mutagenesis of F282 to alanine (F282A)[1].
| Catalog Number | I009578 |
| CAS Number | 1338259-05-4 |
| Synonyms | 2-[4-[[2,3-dimethyl-5-[[(1S)-1-(4-nitrophenyl)ethyl]carbamoyl]indol-1-yl]methyl]phenyl]benzoic acid |
| Molecular Formula | C33H29N3O5 |
| Purity | ≥95% |
| 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 |
| InChIKey | IIJDFXNUWZTHIM-NRFANRHFSA-N |
| SMILES | CC1=C(N(C2=C1C=C(C=C2)C(=O)NC(C)C3=CC=C(C=C3)[N+](=O)[O-])CC4=CC=C(C=C4)C5=CC=CC=C5C(=O)O)C |
| Reference | [1]. Marciano DP, Kuruvilla DS, Boregowda SV, et al. Pharmacological repression of PPARγ promotes osteogenesis. Nat Commun. 2015;6:7443. Published 2015 Jun 12. [2]. Choi JH, et al. Antidiabetic actions of a non-agonist PPARγ ligand blocking Cdk5-mediated phosphorylation. Nature. 2011;477(7365):477-481. Published 2011 Sep 4. |
