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GW6471

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Chemical Structure| 880635-03-0 同义名 : -
CAS号 : 880635-03-0
货号 : A408992
分子式 : C35H36F3N3O4
纯度 : 99%+
分子量 : 619.673
MDL号 : MFCD07784503
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 85 mg/mL(137.17 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • PPARα

    PPARα, IC50:0.24 μM
描述 The peroxisome proliferator-activated receptor alpha (PPARα) is a transcription factor that regulates hepatic fatty acid metabolism. GW 6471 is a potent PPARα antagonist with an IC50 value of 0.24μM.[1] The application of GW6471 (1×10-5mol/L) prevented embryoid bodies from cardiomyocyte differentiation and reduced the expression of α-actinin and troponin-T. GW6471 treatment also tended to decrease the levels of α-MHC and MLC2v in embryoid bodies compared with the controls.[2] Administration of GW 6471 (4 and 10μg/mouse, via intracerebroventricular route; or 1mg/kg, via intraperitoneal route) prevented the anticonvulsant effect of docosahexaenoic acid and the increase in seizure threshold in mice in a dose-dependent manner.[3]
作用机制 GW6471 is a PPARα antagonist. It disrupts the interactions between PPARα and its coactivators, such as steroid receptor coactivator-1 and CREB-binding protein, but promotes the binding of the co-repressors, such as silencing mediator for retinoid and thyroid hormone receptors and nuclear co-repressor.[1]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.61mL

0.32mL

0.16mL

8.07mL

1.61mL

0.81mL

16.14mL

3.23mL

1.61mL
参考文献

[1]Xu HE, Stanley TB, Montana VG, Lambert MH, Shearer BG, Cobb JE, McKee DD, Galardi CM, Plunket KD, Nolte RT, Parks DJ, Moore JT, Kliewer SA, Willson TM, Stimmel JB. Structural basis for antagonist-mediated recruitment of nuclear co-repressors by PPARalpha. Nature. 2002 Feb 14;415(6873):813-7. doi: 10.1038/415813a

[2]Ding L, Liang XG, Lou YJ. Time-dependence of cardiomyocyte differentiation disturbed by peroxisome proliferator-activated receptor alpha inhibitor GW6471 in murine embryonic stem cells in vitro. Acta Pharmacol Sin. 2007 May;28(5):634-42. doi: 10.1111/j.1745-7254.2007.00558.x

[3]Gavzan H, Hashemi F, Babaei J, Sayyah M. A role for peroxisome proliferator-activated receptor α in anticonvulsant activity of docosahexaenoic acid against seizures induced by pentylenetetrazole. Neurosci Lett. 2018 Aug 10;681:83-86. doi: 10.1016/j.neulet.2018.05.042