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Submit ReviewGW 9662
说明： Selective covalent PPARγ antagonist
化学名： 2-Chloro-5-nitro-N-phenylbenzamide
纯度： ≥98% (HPLC)
生物活性 for GW 9662
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.
化合物库 for GW 9662
GW 9662 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for GW 9662
| 分子量 | 276.68 |
| 公式 | C13H9N2O3Cl |
| 储存 | Store at RT |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for GW 9662
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| ethanol | 6.92 | 25 温和加热 | |
| DMSO | 27.67 | 100 |
制备储备液 for GW 9662
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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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产品说明书 for GW 9662
参考文献 for GW 9662
参考文献是支持产品生物活性的出版物。
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
If you know of a relevant reference for GW 9662, please let us know.
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关键词: GW 9662, GW 9662 supplier, Selective, PPARγ, PPARgamma, antagonists, Peroxisome, Proliferator-activating, Receptors, PPAR, GW9662, hematopoietic, haematopoietic, stem, cells, HSC, Hematopoietic, Stem, Cells, 1508, Tocris Bioscience
14 篇 GW 9662 的引用文献
引用文献是使用了 Tocris 产品的出版物。 GW 9662 的部分引用包括：
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
Ali et al (2006) Role of nuclear receptor signaling in platelets: antithrombotic effects of PPARβ. J Neuroinflammation 20 326 PMID: 16368717
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
Esposito et al (2011) Cannabidiol reduces Aβ-induced neuroinflammation and promotes hippocampal neurogenesis through PPARγ involvement. FASEB J 6 e28668 PMID: 22163051
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
Dos-Santos-Pereira et al (2020) Cannabidiol prevents LPS-induced microglial inflammation by inhibiting ROS/NF-κB-dependent signaling and glucose consumption. Glia 68 561 PMID: 31647138
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
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
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
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
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
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GW 9662 的评论
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GW 9662 partially inhibits 15d-PGJ2-mediated pp42/44 activation..
By
Chintan Koyani on 12/10/2018
分析类型： In Vitro
种属： Mouse
细胞系/组织： 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.
