T0070907

The peroxisome proliferator-activated receptor-gamma (PPARgamma) is the nuclear receptor responsible for transducing the therapeutic activity of the thiazolidinediones (TZDs). TZDs are a group of structurally related synthetic PPARgamma receptor agonists with antidiabetic actions in vivo. There are many PPARgamma agonists, including 15-deoxy-Delta12,14-prostaglandin J2 and azelaoyl PAF, which are naturally derived. However, only a few antagonists have been reported. T0070907 is a potent and selective antagonist of the human PPARgamma with an apparent IC50 of 1 nM for the binding inhibition of rosiglitazone, a reference TZD. T0070907 covalently binds to Cys313 of PPARgamma, inducing conformational changes that block the recruitment of transcriptional cofactors to the PPARgamma/RXR heterodimer.Formal Name: 2-chloro-5-nitro-N-4-pyridinyl-benzamide. CAS Number: 313516-66-4. Molecular Formula: C12H8ClN3O3. Formula Weight: 277.7. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMF:PBS (pH 7.2) (1:4): .2 mg/ml, DMSO: 10 mg/ml. lambdamax: 257 nm. SMILES: ClC1=CC=C([N+]([O-])=O)C=C1C(NC2=CC=NC=C2)=O. InChi Code: InChI=1S/C12H8ClN3O3/c13-11-2-1-9(16(18)19)7-10(11)12(17)15-8-3-5-14-6-4-8/h1-7H,(H,14,15,17). InChi Key: FRPJSHKMZHWJBE-UHFFFAOYSA-N.