370700
GW9662 - CAS 22978-25-2 - Calbiochem
Synonym(e):
2-Chloro-5-nitro-N-phenylbenzamide
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Unterstützung erhaltenassay
≥95% (HPLC)
form
crystalline solid
solubility
DMSO: 20 mg/mL, methanol: soluble
General description
A cell-permeable, selective and irreversible PPARγ antagonist (IC50 = 3.3 nM, 32 nM, and 2 μM for PPARγ, PPARα, and PPARδ, respectively). Reported to covalently modify a cysteine residue in the binding site of PPAR. At a concentration of 10 μM, also acts as an agonist of human pregnane X receptor (PXR) and farnesoid X receptor (FXR). Does not activate liver X receptor-α (LXRα), retinoic acid receptor (RAR), retinoid X receptor-α (RXRα) and thyroid receptors α and β (TRα and TRβ).
Biochem/physiol Actions
Target IC50:3.3 nM, 32 nM, and 2 μM for PPARγ, PPARα, and PPARΔ
Preparation Note
Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Lagerklasse
10-13 - German Storage Class 10 to 13
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The PPARs: from orphan receptors to drug discovery.
T M Willson et al.
Journal of medicinal chemistry, 43(4), 527-550 (2000-02-26)
Lisa M Leesnitzer et al.
Biochemistry, 41(21), 6640-6650 (2002-05-23)
In the course of a high throughput screen to search for ligands of peroxisome proliferator activated receptor-gamma (PPARgamma), we identified GW9662 using a competition binding assay against the human ligand binding domain. GW9662 had nanomolar IC(50) versus PPARgamma and was
J T Huang et al.
Nature, 400(6742), 378-382 (1999-08-04)
The peroxisome proliferator-activated receptor-gamma (PPAR-gamma) is a ligand-dependent nuclear receptor that has been implicated in the modulation of critical aspects of development and homeostasis, including adipocyte differentiation, glucose metabolism and macrophage development and function. PPAR-gamma is activated by a range