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575305 T0070907 - CAS 313516-66-4 - Calbiochem

575305
  
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
313516-66-4C₁₂H₈ClN₃O₃
Description
OverviewA 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.
Catalogue Number575305
Brand Family Calbiochem®
Synonyms2-Chloro-5-nitro-N-(4-pyridyl)benzamide
References
ReferencesLee, G., et al. 2002. J. Biol. Chem. 277, 19649.
Product Information
CAS number313516-66-4
ATP CompetitiveN
FormWhite solid
Hill FormulaC₁₂H₈ClN₃O₃
Chemical formulaC₁₂H₈ClN₃O₃
ReversibleN
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetPPARγ
Primary Target K<sub>i</sub>1 nM for PPARγ
Purity≥97% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Carcinogenic / Teratogenic
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
575305 0

Documentation

T0070907 - CAS 313516-66-4 - Calbiochem MSDS

Title

Safety Data Sheet (SDS) 

T0070907 - CAS 313516-66-4 - Calbiochem Certificates of Analysis

TitleLot Number
575305

References

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

Citations

Title
  • Iwona Bogacka, et al. (2005) Structural and functional consequences of mitochondrial biogenesis in human adipocytes in vitro. Journal of Clinical Endocrinology and Metabolism in press,.
  • Data Sheet

    Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

    Revision12-September-2008 RFH
    Synonyms2-Chloro-5-nitro-N-(4-pyridyl)benzamide
    DescriptionA 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.
    FormWhite solid
    Intert gas (Yes/No) Packaged under inert gas
    CAS number313516-66-4
    Chemical formulaC₁₂H₈ClN₃O₃
    Structure formulaStructure formula
    Purity≥97% by HPLC
    SolubilityDMSO (5 mg/ml)
    Storage Protect from light
    +2°C to +8°C
    Do Not Freeze Ok to freeze
    Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
    Toxicity Carcinogenic / Teratogenic
    ReferencesLee, G., et al. 2002. J. Biol. Chem. 277, 19649.
    Citation
  • Iwona Bogacka, et al. (2005) Structural and functional consequences of mitochondrial biogenesis in human adipocytes in vitro. Journal of Clinical Endocrinology and Metabolism in press,.