T0070907 , ≥99% , 313516-66-4

Synonym(s):
2-Chloro-5-nitro-N-(4-pyridyl)benzamide;2-Chloro-5-nitro-N-4-pyridinyl-benzamide;Benzamide, 2-chloro-5-nitro-N-4-pyridinyl-;T0070907 - CAS 313516-66-4 - Calbiochem

CAS NO.：313516-66-4

Empirical Formula: C12H8ClN3O3

Molecular Weight: 277.66

MDL number: MFCD00121849

PRODUCT Properties

• Melting point: >184°C (dec.)
• Density: 1.498
• storage temp.: 2-8°C
• solubility: DMSO: >10mg/mL
• form: White solid
• color: white
• Water Solubility: Soluble in DMSO at 10mg/ml. Insoluble in water.
• Sensitive: Light Sensitive
• 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)
• InChIKey: FRPJSHKMZHWJBE-UHFFFAOYSA-N
• SMILES: [O-][N+](=O)c1ccc(Cl)c(c1)C(=O)Nc2ccncc2

Description and Uses

The peroxisome proliferator-activated receptor-γ (PPARγ) is the nuclear receptor responsible for transducing the therapeutic activity of the thiazolidinediones (TZDs). TZDs are a group of structurally related synthetic PPARγ receptor agonists with antidiabetic actions in vivo. There are many PPARγ agonists, including 15-deoxy-Δ^12,14-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 PPARγ with an apparent IC₅₀ of 1 nM for the binding inhibition of rosiglitazone, a reference TZD. T0070907 covalently binds to Cys³¹³ of PPARγ, inducing conformational changes that block the recruitment of transcriptional cofactors to the PPARγ/RXR heterodimer.

A cell-permeable chloro-nitro-benzamido compound that acts as a potent, specific, irreversible, and high-affinity antagonist of PPAR with a Ki of 1 nM. Displays >800-fold greater selectivity for PPAR over PPARa and PPARd (Ki = 0.85 and 1.8 ,

Safety

• Symbol(GHS): GHS07
• Signal word: Warning
• Hazard statements: H315-H335-H302-H319
• Precautionary statements: P305+P351+P338-P261-P280a-P304+P340-P405-P501a
• PPE: dust mask type N95 (US), Eyeshields, Gloves
• Hazard Codes: Xn
• Risk Statements: 22-36
• Safety Statements: 26
• WGK Germany: 2
• HS Code: 29333990
• Storage Class: 11 - Combustible Solids