Home / PPAR gamma Receptor Antagonists / GW 9662

GW 9662

Catalog #: 1508
14 Citations 2 Reviews Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
1508/10
1508/50
GW 9662 | CAS No. 22978-25-2 | PPAR gamma Receptor Antagonists
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Description: Selective covalent PPARγ antagonist

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

Purity: ≥98%

Product Details
Citations (14)
Supplemental Products
Reviews (2)
Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

GW 9662 is a 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. Anticancer, inhibits growth of human mammary tumor cell lines.

Technical Data

M.Wt:
276.68
Formula:
C13H9N2O3Cl
Solubility:
Soluble to 25 mM in ethanol with gentle warming and to 100 mM in DMSO
Purity:
≥98%
Storage:
Store at RT
CAS No:
22978-25-2

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.

Background References

  1. Telmisartan activates endothelial nitric oxide synthase via Ser1177 phosphorylation in vascular endothelial cells.
    Myojo, Masahiro, Nagata, Daisuke, Fujita, Daishi, Kiyosue, Arihiro, Takahashi, Masao, Satonaka, Hiroshi, Morishita, Yoshiyuk, Akimoto, Tetsu, Nagai, Ryozo, Komuro, Issei, Hirata, Yasunobu
    PLoS ONE, 2014;9(5):e96948.
  2. Different immune cells mediate mechanical pain hypersensitivity in male and female mice.
    Sorge R, Mapplebeck J, Rosen S, Beggs S, Taves S, Alexander J, Martin L, Austin J, Sotocinal S, Chen D, Yang M, Shi X, Huang H, Pillon N, Bilan P, Tu Y, Klip A, Ji R, Zhang J, Salter M, Mogil J
    Nat Neurosci, 2015;18(8):1081-3.
  3. Role of retinal pigment epithelial cell beta-catenin signaling in experimental proliferative vitreoretinopathy.
    Umazume K, Tsukahara R, Liu L, Fernandez de Castro J, McDonald K, Kaplan H, Tamiya S
    Am J Pathol, 2014;184(5):1419-28.
  4. Additive Renoprotection by Pioglitazone and Fenofibrate against Inflammatory, Oxidative and Apoptotic Manifestations of Cisplatin Nephrotoxicity: Modulation by PPARs.
    Helmy M, Helmy M, El-Mas M
    PLoS ONE, 2015;10(11):e0142303.
  5. IL-4 inhibits osteoclast formation through a direct action on osteoclast precursors via peroxisome proliferator-activated receptor γ1.
    Bendixen et al.
    Proc.Natl.Acad.Sci.U.S.A., 2001;98:2443
  6. Functional consequences of cysteine modification in the ligand binding sites of peroxisone proliferator activated receptors by GW9662.
    Leesnitzer et al.
    Biochemistry, 2002;41:6640
  7. 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.
    Seargent et al.
    Br.J.Pharmacol., 2004;143:933

Product Datasheets

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Citations for GW 9662

The citations listed below are publications that use Tocris products. Selected citations for GW 9662 include:

14 Citations: Showing 1 - 10

  1. Cannabidiol prevents LPS-induced microglial inflammation by inhibiting ROS/NF-κB-dependent signaling and glucose consumption.
    Authors: Dos-Santos-Pereira Et al.
    Glia  2020;68:561
  2. Identification and characterization of a novel anti-inflammatory lipid isolated from Mycobacterium vaccae, a soil-derived bacterium with immunoregulatory and stress resilience properties.
    Authors: Smith Et al.
    Psychopharmacology (Berl)  2019;
  3. Antagonism of PPAR-γ signaling expands human hematopoietic stem and progenitor cells by enhancing glycolysis.
    Authors: Guo Et al.
    Nat Med  2018;24:360
  4. 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.
    Authors: Kotla and Rao
    J Biol Chem  2015;290:30306
  5. Additive Renoprotection by pioglit. and fenofi. against Inflammatory, Oxidative and Apoptotic Manifestations of cisp. Nephrotoxicity: Modulation by PPARs.
    Authors: Helmy Et al.
    PLoS One  2015;10:e0142303
  6. Mechanisms of Nifedipine-Downregulated CD40L/sCD40L Signaling in Collagen Stimulated Human Platelets.
    Authors: Chen Et al.
    PLoS One  2015;10:e0127054
  7. Antiplatelet activity of nifed. is mediated by inhibition of NF-κB activation caused by enhancement of PPAR-β/-γ activity.
    Authors: Shih Et al.
    Br J Pharmacol  2014;171:1490
  8. Palmitoylethanolamide exerts neuroprotective effects in mixed neuroglial cultures and organotypic hippocampal slices via peroxisome proliferator-activated receptor-α.
    Authors: Scuderi Et al.
    Arterioscler Thromb Vasc Biol  2012;9:49
  9. Isorhamnetin inhibits proliferation and invasion and induces apoptosis through the modulation of peroxisome proliferator-activated receptor γ activation pathway in gastric cancer.
    Authors: Ramachandran Et al.
    J Biol Chem  2012;287:38028
  10. Lipolytic products activate peroxisome proliferator-activated receptor (PPAR) α and δ in brown adipocytes to match fatty acid oxidation with supply.
    Authors: Mottillo Et al.
    PLoS One  2012;287:25038

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Reviews for GW 9662

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Great GW 9662
By Anonymous on 12/05/2021
Species: Mouse

GW 9662 at 2microM was used to test its effect on EC sprouting.

Great GW 9662 1508
PPARy in m1 m2 macrophages
By Anonymous on 09/24/2019
Species: Mouse

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

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