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.

• Sinonimo/i: T0070907, 2-Chloro-5-nitro-N-(4-pyridyl)benzamide
• Formula empirica (notazione di Hill): C₁₂H₈ClN₃O₃
• Numero CAS: 313516-66-4
• Peso molecolare: 277.66
• Numero MDL: MFCD00121849
• Codice UNSPSC: 12352200

Proprietà

• Saggio: ≥97% (HPLC)
• Forma fisica: solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; protect from light
• Colore: white
• Solubilità: DMSO: 5 mg/mL
• Temperatura di conservazione: 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); FRPJSHKMZHWJBE-UHFFFAOYSA-N

Descrizione

Descrizione generale

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.

Azioni biochim/fisiol

Primary Target
PPARγ

Target K_i: 1 nM for PPARγ

Attenzione

Toxicity: Carcinogenic / Teratogenic (D)

Ricostituzione

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

Altre note

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

Note legali

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

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 2