575305-M

T0070907

A cell-permeable chloro-nitro-benzamido compound that acts as a potent, specific, irreversible, and high-affinity antagonist of PPARγ with a K_i of 1 nM.

• Synonyme(s) : T0070907, 2-Chloro-5-nitro-N-(4-pyridyl)benzamide
• Formule empirique (notation de Hill): C₁₂H₈ClN₃O₃
• Numéro CAS: 313516-66-4
• Poids moléculaire : 277.66
• Numéro MDL: MFCD00121849
• Code UNSPSC : 12352200

Propriétés

• Pureté: ≥97% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: white
• Solubilité: DMSO: 5 mg/mL
• Température de stockage: 2-8°C
• 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)
• Clé InChI: FRPJSHKMZHWJBE-UHFFFAOYSA-N

Description

Description générale

A cell-permeable chloro-nitro-benzamido compound that acts as a potent, specific, irreversible, and high-affinity antagonist of PPARγ with a K_i of 1 nM. Displays >800-fold greater selectivity for PPARγ over PPARα and PPARδ (K_i = 0.85 µM and 1.8 µM, respectively). Blocks hormone- and agonist-induced adipogenesis in 3T3-L1 cells. It suppresses interactions between PPARγ and coactivator-derived peptides, while promotes the recruitment of corepressor-derived peptides. Shown to modulate the interaction of PPARγ2 with the cofactor proteins through covalent binding to Cys³¹³ in its ligand-binding domain.

A cell-permeable, potent, specific, irreversible, and high-affinity antagonist of PPARγ (K_i = 1 nM). Reported to be >800-fold more specific for PPARγ compared to PPARα (K_i = 850 nM) and PPARδ (K_i = 1.8 µM). Shown to block hormone- and agonist-induced adipogenesis in 3T3-L1 cells. Suppresses interactions between PPARγ and coactivator-derived peptides while promoting the recruitment of co-repressor-derived peptides. Also shown to modulate the interaction of PPARγ2 with cofactor proteins through covalent binding to Cys³¹³ in the ligand-binding domain.

Actions biochimiques/physiologiques

Primary Target
PPARγ

Target K_i: 1 nM for PPARγ

Avertissement

Toxicity: Carcinogenic / Teratogenic (D)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Autres remarques

Lee, G., et al. 2002. J. Biol. Chem.277, 19649.

Informations légales

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 2