GW 0742

Pricing Availability   Qty
说明: Highly selective, potent PPARδ agonist
化学名: [4-[[[2-[3-Fluoro-4-(trifluoromethyl)phenyl]-4-methyl-5-thiazolyl]methyl]thio]-2-methylphenoxy]acetic acid
纯度: ≥98% (HPLC)
说明书
引用文献 (14)
评论

生物活性 for GW 0742

GW 0742 is a potent and highly selective PPARδ agonist. EC50 values are 0.001, 1.1 and 2 μM for transactivation of human PPARδ, -α, and -γ receptors respectively. Neuroprotective in rat cerebellar granule neuronal cultures after brief (12-hour) exposure but exhibits inherent toxicity after prolonged (48-hour) incubation. Increases rate of fatty acid oxidation and protects against ischemia/reperfusion injury in neonatal and adult cardiomyocytes.

许可信息

Sold for research purposes under agreement from GlaxoSmithKline

化合物库 for GW 0742

GW 0742 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 0742

分子量 471.49
公式 C21H17F4NO3S2
储存 Desiccate at +4°C
纯度 ≥98% (HPLC)
CAS Number 317318-84-6
PubChem ID 9934458
InChI Key HWVNEWGKWRGSRK-UHFFFAOYSA-N
Smiles CC1=C(CSC2=CC(C)=C(OCC(O)=O)C=C2)SC(=N1)C1=CC(F)=C(C=C1)C(F)(F)F

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 0742

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
ethanol 24.23 50
DMSO 48.5 100

制备储备液 for GW 0742

以下数据基于产品分子量 471.49。 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.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 2.12 mL 10.6 mL 21.21 mL
5 mM 0.42 mL 2.12 mL 4.24 mL
10 mM 0.21 mL 1.06 mL 2.12 mL
50 mM 0.04 mL 0.21 mL 0.42 mL

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产品说明书 for GW 0742

分析证书/产品说明书
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参考文献 for GW 0742

参考文献是支持产品生物活性的出版物。

Sznaidman et al (2003) Novel selective small molecule agonists for peroxisome proliferator-activated receptor δ (PPARδ) - Synthesis and biological activity. Bioorg.Med.Chem.Lett. 13 1517 PMID: 12699745

Smith et al (2004) Effect of the peroxisome proliferator-activated receptor β activator GW0742 in rat cultured cerebellar granule neurons. J.Neurosci.Res. 77 240 PMID: 15211590

Yue et al (2008) In vivo activation of peroxisome proliferator-activayed receptor-δ protects the heart from ischemia/reperfusion injury in Zucker fatty rats. J.Pharm.Exp.Ther. 325 466


If you know of a relevant reference for GW 0742, please let us know.

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关键词: GW 0742, GW 0742 supplier, selective, potent, PPARδ, PPARdelta, agonists, Peroxisome, Proliferator-activating, Receptors, GW0742, GlaxoSmithKline, GSK, 2229, Tocris Bioscience

14 篇 GW 0742 的引用文献

引用文献是使用了 Tocris 产品的出版物。 GW 0742 的部分引用包括:

Hatano et al (2010) Murine atopic dermatitis responds to peroxisome proliferator-activated receptors α and β/δ (but not γ) and liver X receptor activators. PLoS One 125 160 PMID: 19818482

Niu et al (2015) Development of PPAR-agonist GW0742 as antidiabetic drug: study in animals. Invest Ophthalmol Vis Sci 9 5625 PMID: 26508837

Tsai et al (2014) Decrease of PPARδ in Type-1-Like Diabetic Rat for Higher Mortality after Spinal Cord Injury. PPAR Res 2014 456386 PMID: 24817882

Perez-Schindler et al (2014) The coactivator PGC-1α regulates skeletal muscle oxidative metabolism independently of the nuclear receptor PPARβ/δ in sedentary mice fed a regular chow diet. Diabetologia 57 2405 PMID: 25116175

Qian et al (2015) Peroxisomes in Different Skeletal Cell Types during Intramembranous and Endochondral Ossification and Their Regulation during Osteoblast Differentiation by Distinct Peroxisome Proliferator-Activated Receptors. PLoS One 10 e0143439 PMID: 26630504

Capozzi et al (2013) Peroxisome proliferator-activated receptor-β/δ regulates angiogenic cell behaviors and oxygen-induced retinopathy. J Allergy Clin Immunol 54 4197 PMID: 23716627

Teske et al (2014) Modulation of Transcription mediated by the Vitamin D Receptor and the Peroxisome Proliferator-Activated Receptor δ in the presence of GW0742 analogs. Drug Des Devel Ther 3 PMID: 25485183

Martín-Martín et al (2018) PPARδ Elicits Ligand-Independent Repression of Trefoil Factor Family to Limit Prostate Cancer Growth. Cancer Res 78 399 PMID: 29187400

Batista et al (2012) Structural insights into human peroxisome proliferator activated receptor delta (PPAR-delta) selective ligand binding. PLoS One 7 e33643 PMID: 22606221

Tian et al (2012) PPARδ activation protects endothelial function in diabetic mice. Diabetes 61 3285 PMID: 22933110

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

Wang et al (2017) Retinoic acid inhibits white adipogenesis by disrupting GADD45A-mediated Zfp423 DNA demethylation. J Mol Cell Biol 9 338 PMID: 28992291

Zhang (2017) PPARD is an Inhibitor of Cartilage Growth in External Ears Int J Biol Sci 13 669 PMID: 28539839

Halstead et al (2017) Bladder-cancer-associated mutations in RXRA activate peroxisome proliferator-activated receptors to drive urothelial proliferation. Elife 6 PMID: 29143738


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