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 Ki of 1 nM.
Synonym(s):
T0070907, 2-Chloro-5-nitro-N-(4-pyridyl)benzamide
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About This Item
Empirical Formula (Hill Notation):
C12H8ClN3O3
CAS Number:
Molecular Weight:
277.66
MDL number:
UNSPSC Code:
12352200
Recommended Products
Assay
≥97% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
white
solubility
DMSO: 5 mg/mL
storage temp.
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
General description
A cell-permeable chloro-nitro-benzamido compound that acts as a potent, specific, irreversible, and high-affinity antagonist of PPARγ with a Ki of 1 nM. Displays >800-fold greater selectivity for PPARγ over PPARα and PPARδ (Ki = 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 (Ki = 1 nM). Reported to be >800-fold more specific for PPARγ compared to PPARα (Ki = 850 nM) and PPARδ (Ki = 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.
Biochem/physiol Actions
Primary Target
PPARγ
PPARγ
Target Ki: 1 nM for PPARγ
Warning
Toxicity: Carcinogenic / Teratogenic (D)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Lee, G., et al. 2002. J. Biol. Chem.277, 19649.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 2
Certificates of Analysis (COA)
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