SR 1664

Apart from direct peroxisome proliferator-activated receptor gamma (PPARgamma) agonism, several PPARgamma ligands have recently been shown to exert anti-diabetic effects through a second, distinct biochemical function: blocking the obesity-linked phosphorylation of PPARgamma by cyclin-dependent kinase 5 (Cdk5) at serine 273. This effect requires binding to the PPARgamma ligand binding domain, which causes a conformational change that interferes with the ability of Cdk5 to phosphorylate serine 273. SR 1664 is a small molecule that blocks phosphorylation of peroxisome proliferator-activated receptor gamma (PPARgamma) by cyclin-dependent kinase 5 with an IC50 value of 80 nM (Ki = 28.7 nM) without exhibiting agonist activity at the PPARgamma receptor. It demonstrates potent, dose-dependent anti-diabetic effects in obese mice without inducing fluid retention and weight gain or inhibiting bone formation.Formal Name: 4'-[[2,3-dimethyl-5-[[[(1S)-1-(4-nitrophenyl)ethyl]amino]carbonyl]-1H-indol-1-yl]methyl]-[1,1'-biphenyl]-2-carboxylic acid. CAS Number: 1338259-05-4. Molecular Formula: C33H29N3O5. Formula Weight: 547.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 15 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml, Ethanol: 15 mg/ml. lambdamax: 252 nm. SMILES: C[C@H](NC(C1=CC=C(N(CC2=CC=C(C3=CC=CC=C3C(O)=O)C=C2)C(C)=C4C)C4=C1)=O)C5=CC=C([N+]([O-])=O)C=C5. InChi Code: 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. InChi Key: IIJDFXNUWZTHIM-NRFANRHFSA-N.