GW 9662

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Cat.No. 1508 - GW 9662 | C13H9N2O3Cl | CAS No. 22978-25-2
Description: Selective covalent PPARγ antagonist
Chemical Name: 2-Chloro-5-nitro-N-phenylbenzamide
Purity: ≥98% (HPLC)
Datasheet
Citations (13)
Reviews (2)
Literature (4)

Biological Activity

Selective irreversible PPARγ antagonist (IC50 values are 3.3, 32 and 2000 nM for PPARγ, PPARα and PPARδ respectively). Blocks the inhibition of osteoclast formation induced by IL-4 in the low micromolar range (1-2 μM), therefore is more potent than BADGE (Cat. No. 1326). Anticancer, inhibits growth of human mammary tumor cell lines.

Technical Data

M. Wt 276.68
Formula C13H9N2O3Cl
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 22978-25-2
PubChem ID 644213
InChI Key DNTSIBUQMRRYIU-UHFFFAOYSA-N
Smiles [O-][N+](=O)C1=CC(C(=O)NC2=CC=CC=C2)=C(Cl)C=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
ethanol 6.92 25 with gentle warming
DMSO 27.67 100

Preparing Stock Solutions

The following data is based on the product molecular weight 276.68. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.61 mL 18.07 mL 36.14 mL
5 mM 0.72 mL 3.61 mL 7.23 mL
10 mM 0.36 mL 1.81 mL 3.61 mL
50 mM 0.07 mL 0.36 mL 0.72 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

References are publications that support the biological activity of the product.

Bendixen et al (2001) IL-4 inhibits osteoclast formation through a direct action on osteoclast precursors via peroxisome proliferator-activated receptor γ1. Proc.Natl.Acad.Sci.U.S.A. 98 2443 PMID: 11226258

Leesnitzer et al (2002) Functional consequences of cysteine modification in the ligand binding sites of peroxisone proliferator activated receptors by GW9662. Biochemistry 41 6640 PMID: 12022867

Seargent et al (2004) GW9662, a potent antaognist of PPARγ, inhibits growth of breast tumour cells and promotes the anticancer effects of the PPARγ agonist rosiglitazone, independently of PPARγ activation. Br.J.Pharmacol. 143 933 PMID: 15533890


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Keywords: GW 9662, GW 9662 supplier, Selective, PPARγ, PPARgamma, antagonists, Peroxisome, Proliferator-activating, Receptors, PPAR, GW9662, 1508, Tocris Bioscience

13 Citations for GW 9662

Citations are publications that use Tocris products. Selected citations for GW 9662 include:

Shih et al (2014) Antiplatelet activity of nifed. is mediated by inhibition of NF-κB activation caused by enhancement of PPAR-β/-γ activity. Br J Pharmacol 171 1490 PMID: 24730061

Ramachandran et al (2012) Isorhamnetin inhibits proliferation and invasion and induces apoptosis through the modulation of peroxisome proliferator-activated receptor γ activation pathway in gastric cancer. J Biol Chem 287 38028 PMID: 22992727

Smith et al (2019) Identification and characterization of a novel anti-inflammatory lipid isolated from Mycobacterium vaccae, a soil-derived bacterium with immunoregulatory and stress resilience properties. Psychopharmacology (Berl) PMID: 31119329

Helmy et al (2015) Additive Renoprotection by pioglit. and fenofi. against Inflammatory, Oxidative and Apoptotic Manifestations of cisp. Nephrotoxicity: Modulation by PPARs. PLoS One 10 e0142303 PMID: 26536032

Chen et al (2015) Mechanisms of Nifedipine-Downregulated CD40L/sCD40L Signaling in Collagen Stimulated Human Platelets. PLoS One 10 e0127054 PMID: 25970603

Kotla and Rao (2015) Reactive Oxygen Species (ROS) Mediate p300-dependent STAT1 Protein Interaction with Peroxisome Proliferator-activated Receptor (PPAR)-γ in CD36 Protein Expression and Foam Cell Formation. J Biol Chem 290 30306 PMID: 26504087

Ali et al (2009) Antiplatelet actions of STAT and fibrates are mediated by PPARs. J Neurosci 29 706 PMID: 19150877

Guo et al (2018) Antagonism of PPAR-γ signaling expands human hematopoietic stem and progenitor cells by enhancing glycolysis. Nat Med 24 360 PMID: 29377004

Postea et al (2008) Homocysteine up-regulates vascular transmembrane chemokine CXCL16 and induces CXCR6+ lymphocyte recruitment in vitro and in vivo. J Cell Mol Med 12 1700 PMID: 18194461

Mottillo et al (2012) Lipolytic products activate peroxisome proliferator-activated receptor (PPAR) α and δ in brown adipocytes to match fatty acid oxidation with supply. PLoS One 287 25038 PMID: 22685301

Scuderi et al (2012) Palmitoylethanolamide exerts neuroprotective effects in mixed neuroglial cultures and organotypic hippocampal slices via peroxisome proliferator-activated receptor-α. Arterioscler Thromb Vasc Biol 9 49 PMID: 22405189

Ali et al (2006) Role of nuclear receptor signaling in platelets: antithrombotic effects of PPARβ. J Neuroinflammation 20 326 PMID: 16368717

Esposito et al (2011) Cannabidiol reduces Aβ-induced neuroinflammation and promotes hippocampal neurogenesis through PPARγ involvement. FASEB J 6 e28668 PMID: 22163051


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Reviews for GW 9662

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PPARy in m1 m2 macrophages.
By Anonymous on 09/24/2019
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: macrophage

Used this produce in mouse macrophages to inhibit ppar gamma at 1um. worked very well


GW 9662 partially inhibits 15d-PGJ2-mediated pp42/44 activation..
By Chintan Koyani on 12/10/2018
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: HL-1 cardiomyocytes

HL-1 cardiomyocytes were incubated with GW 9662 (2 µM) for 30 min prior to addition of 15 µM 15d-PGJ2 for 30 min. Preincubation of cells with GW 9662 partially abolished activation of p42/44 MAPK, while Tesaglitazar and T 0070907 inhibited the activation completely.

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