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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.
This website uses cookies, which are necessary for the technical operation of the website and are always set. Other cookies, which increase the usability of this website, serve for direct advertising or simplify interaction with other websites and social networks, will only be used with your consent.
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