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370700

GW9662 - CAS 22978-25-2 - Calbiochem

Name: GW9662 - CAS 22978-25-2 - Calbiochem
Brand: MM

别名:

2-Chloro-5-nitro-N-phenylbenzamide

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属性

assay

≥95% (HPLC)

form

crystalline solid

solubility

DMSO: 20 mg/mL, methanol: soluble

说明

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 (LXR_α), retinoic acid receptor (RAR), retinoid X receptor-α (RXR_α) and thyroid receptors α and β (TR_α and TR_β).

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.

存储类别

10-13 - German Storage Class 10 to 13

法规信息

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Functional consequences of cysteine modification in the ligand binding sites of peroxisome proliferator activated receptors by GW9662.

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

The PPARs: from orphan receptors to drug discovery.

T M Willson et al.

Journal of medicinal chemistry, 43(4), 527-550 (2000-02-26)

Interleukin-4-dependent production of PPAR-gamma ligands in macrophages by 12/15-lipoxygenase.

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