GW-9662


Catalog No. size PriceQuantity
M6711-2 2mg solid $86
M6711-10 10mg solid $360

Description

Cas:22978-25-2

Product Information

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.

 

Chemical Formula: C13H9ClN2O3

 

Exact Mass: 276.03017

 

Molecular Weight: 276.67 

 

Elemental Analysis: C, 56.43; H, 3.28; Cl, 12.81; N, 10.13; O, 17.35

 

Synonym: 

 

GW9662

GW-9662

GW 9662

 

Chemical Name:

2-Chloro-5-nitro- N -phenylbenzamide

 

InChi Key:

DNTSIBUQMRRYIU-UHFFFAOYSA-N

 

InChi Code:    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)

 

Smiles Code:

O=C(NC1=CC=CC=C1)C2=CC([N+]([O-])=O)=CC=C2Cl

 

 

Technical Data:

 

Appearance: Solid powder

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

 

In Vitro

GW9662 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. GW9662 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, GW9662 is a potent and selective antagonist of full-length PPARγ. Co-treatment with both 50 μM BRL 49653 and 10 μM GW9662 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 GW9662 (P=0.01) alone.

 

In Vivo

Bone marrow (BM) nucleated cell counts in both BADGE- and GW9662(1 mg/kg, i.p.)-treated mice are significantly higher than counts in the aplastic anemia (AA) group. GW9662 (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.

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