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Submit ReviewTesaglitazar
说明： PPARα/γ agonist
别名： AZ 242
化学名： (S)-2-Ethoxy-3-[4-[2-(4-methanesulfonyloxyphenyl)ethoxy]phenyl]propanoic acid
纯度： ≥98% (HPLC)
生物活性 for Tesaglitazar
Tesaglitazar is a dual-specificity PPARα/γ agonist (IC50 values are 0.35 and 3.8 μM for PPARγ and PPARα respectively). Prevents atherosclerosis progression in E3L.CETP transgenic mice. Also reduces insulin resistance in obese Zucker rats. Orally active.
许可信息
Sold with the permission of AstraZeneca UK Ltd.
技术数据 for Tesaglitazar
| 分子量 | 408.47 |
| 公式 | C20H24O7S |
| 储存 | Desiccate at RT |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 251565-85-2 |
| PubChem ID | 208901 |
| InChI Key | CXGTZJYQWSUFET-IBGZPJMESA-N |
| Smiles | CS(OC1=CC=C(CCOC2=CC=C(C[C@H](OCC)C(O)=O)C=C2)C=C1)(=O)=O |
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 Tesaglitazar
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 40.85 | 100 | |
| ethanol | 40.85 | 100 |
制备储备液 for Tesaglitazar
以下数据基于产品分子量 408.47。 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 | 2.45 mL | 12.24 mL | 24.48 mL |
| 5 mM | 0.49 mL | 2.45 mL | 4.9 mL |
| 10 mM | 0.24 mL | 1.22 mL | 2.45 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.49 mL |
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产品说明书 for Tesaglitazar
参考文献 for Tesaglitazar
参考文献是支持产品生物活性的出版物。
Cronet et al (2001) Structure of the PPARβ and -γ ligand binding domain in complex with AZ 242; ligand selectivity and agonist activation in the PPAR family. Structure 9 699 PMID: 11587644
Ljung et al (2002) AZ 242, a novel PPARα/γ agonist with beneficial effects on Ins resistance and carbohydrate and lipid metabolism in ob/ob mice and obese Zucker rats. J.Lipid Res. 43 1855 PMID: 12401884
Ebdrup et al (2003) Synthesis and biological and structural characterization of the dual-acting peroxisome proliferator-activated receptor α/γ agonist ragaglitazar. J.Med.Chem. 46 1306 PMID: 12672231
van der Hoorn et al (2009) The dual PPARα/γ agonist tesaglitazar blocks progression of pre-existing atherosclerosis in APOE*3Leiden.CETP transgenic mice. Br.J.Pharmacol. 156 1067 PMID: 19220285
If you know of a relevant reference for Tesaglitazar, please let us know.
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关键词: Tesaglitazar, Tesaglitazar supplier, AZ242, peroxisome, proliferator, activated, receptors, ppars, ppara, pparalpha, pparα, pparg, ppargamma, pparγ, agonists, astrazeneca, AZ, 242, Non-selective, PPAR, 3965, Tocris Bioscience
1 篇 Tesaglitazar 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Tesaglitazar 的部分引用包括：
Fellous et al (2020) Phytocannabinoids promote viability and functional adipogenesis of bone marrow-derived mesenchymal stem cells through different molecular targets Biochemical Pharmacology 175 PMID: 32061773
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Tesaglitazar 的评论
平均评分: 5 (Based on 1 Review.)
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Tesaglitazar completely abolishes 15d-PGJ2 induced p42/44 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 Tesaglitazar (10 µM) for 30 min prior to addition of 15 µM 15d-PGJ2 for 30 min. Preincubation of cells with Tesaglitazar completely abolished activation of p42/44 MAPK indicating involvement of PPAR gamma in cellular signalling in response to 15d-PGJ2.
