GW-9662

GW-9662 is a potent, irreversible and selective PPARgamma antagonist, which prevented activation of PPARgamma and inhibited growth of human mammary tumour cell lines. GW-9662 may permit use of anti-ER strategies to inhibit breast cancer in ER- patients.

Product information

CAS Number: 22978-25-2

Molecular Weight: 276.68

Formula: C13H9ClN2O3

Synonym:

GW 9662

GW9662

GW-9662

Chemical Name: 2-Chloro-5-nitro- N -phenylbenzamide

Smiles: [O-][N+](=O)C1=CC(=C(Cl)C=C1)C(=O)NC1C=CC=CC=1

InChiKey: DNTSIBUQMRRYIU-UHFFFAOYSA-N

InChi: InChI=1S/C13H9ClN2O3/c14-12-7-6-10(16(18)19)8-11(12)13(17)15-9-4-2-1-3-5-9/h1-8H,(H,15,17)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO, not in water

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

GW-9662 inhibits radioligand binding to PPARγ, PPARα, and PPARδ with pIC50s of 8.48±0.27 (IC50=3.3 nM; n=10), 7.49±0.17 (IC50=32 nM; n=9), and 5.69±0.17 (IC50=2000 nM; n=3), respectively. GW-9662 has nanomolar IC50 versus PPARγ and is 10- and 600-fold less potent in binding experiments using PPARα and PPARδ, respectively. In cell-based reporter assays, GW-9662 is a potent and selective antagonist of full-length PPARγ. Co-treatment with both 50 μM BRL 49653 and 10 μM GW-9662 results in statistically lower viable cell numbers after 7 days when compared to treatment with either 50 μM BRL 49653 (P=0.001) or 10 μM GW-9662 (P=0.01) alone.

In Vivo:

Bone marrow (BM) nucleated cell counts in both BADGE- and GW-9662(1 mg/kg, i.p.)-treated mice are significantly higher than counts in the aplastic anemia (AA) group. GW-9662 (1 mg/kg, i.p.) largely attenuates the renoprotective effects of Lipopolysaccharide (LPS) in the rat.

References:

1. Jaudszus A, Lorkowski S, Gruen M, Roth A, Jahreis G. Limited Applicability of GW9662 to Elucidate PPARγ-Mediated Fatty Acid Effects in Primary Human T-Helper Cells. Int J Inflam. 2014;2014:149628. doi: 10.1155/2014/149628. Epub 2014 Jun 25. PubMed PMID: 25054074; PubMed Central PMCID: PMC4099290.

Products are for research use only. Not for human use.