T0070907A cell-permeable chloro-nitro-benzamido compound that acts as a potent and specific antagonist of PPARg

T0070907 (CAS 313516-66-4)

T0070907 | CAS 313516-66-4 is rated 5.0 out of 5 by 1.
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Synonym: 2-chloro-5-nitro-N-4-pyridinyl-benzamide
Application: A cell-permeable chloro-nitro-benzamido compound that acts as a potent and specific antagonist of PPARg
CAS Number: 313516-66-4
Purity: >97%
Molecular Weight: 277.7
Molecular Formula: C12H8ClN3O3
* Refer to Certificate of Analysis for lot specific data (including water content).
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T0070907 is 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 PPARg over PPARa and PPARd (Ki = 0.85 μM and 1.8 μM, respectively). Blocks hormone- and agonist-induced adipogenesis in 3T3-L1 cells. It suppresses interactions between PPARg and coactivator-derived peptides, while promotes the recruitment of corepressor-derived peptides. Shown to modulate the interaction of PPARg2 with the cofactor proteins through covalent binding to Cys313 in its ligand-binding domain.


References

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

Physical State :
Solid
Solubility :
Soluble in DMSO (5 mg/ml), and ethanol (<1 mg/ml at 25° C). Insoluble in water.
Storage :
Store at -20° C
Melting Point :
193.12° C (Predicted)
Boiling Point :
~381.7° C at 760 mmHg (Predicted)
Density :
~1.5 g/cm3 (Predicted)
Refractive Index :
n20D 1.68 (Predicted)
IC50 :
PPARγ: IC50 = 1 µM (human)
Ki Data :
PPARγ: Ki= 1 nM; PPARα: Ki= 850 nM; PPARδ: Ki= 1.8 µM
pK Values :
pKa: 10.55 (Predicted), pKb: 5.11 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
2
PubChem CID :
2777391
MDL Number :
MFCD00121849
SMILES :
C1=CC(=C(C=C1[N+](=O)[O-])C(=O)NC2=CC=NC=C2)Cl

Download SDS (MSDS)

Certificate of Analysis

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Rated 5 out of 5 by from Zuckermann et al Zuckermann et al. (PubMed ID 26333042) used T0070907 to inhibit PPAR and prevented downstream -catenin degradation while increasing histone 2/3 acetylation in human hepatocarcinoma cell line (Huh7). -SCBT Publication Review
Date published: 2015-07-08
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