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.

• 동의어(들): T0070907, 2-Chloro-5-nitro-N-(4-pyridyl)benzamide
• 실험식(Hill 표기법): C₁₂H₈ClN₃O₃
• CAS Number: 313516-66-4
• Molecular Weight: 277.66
• MDL number: MFCD00121849
• UNSPSC 코드: 12352200

속성

• 분석: ≥97% (HPLC)
• 양식: solid
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; protect from light
• 색상: white
• solubility: DMSO: 5 mg/mL
• 저장 온도: 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)
• InChI key: FRPJSHKMZHWJBE-UHFFFAOYSA-N

설명

일반 설명

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.

생화학적/생리학적 작용

Primary Target
PPARγ

Target K_i: 1 nM for PPARγ

경고

Toxicity: Carcinogenic / Teratogenic (D)

재구성

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

기타 정보

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

법적 정보

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

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 2