产品说明书

Turofexorate isopropyl

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Chemical Structure| 629664-81-9 同义名 : -
CAS号 : 629664-81-9
货号 : A653721
分子式 : C25H24F2N2O3
纯度 : 98+%
分子量 : 438.466
MDL号 : MFCD13181507
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: 25 mg/mL(57.02 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
描述 Turofexorate isopropyl (WAY-362450) is a potent, selective, and orally bioavailable agonist of the farnesoid X receptor (FXR) with an EC50 of 4 nM[1].
作用机制 WAY-362450 bounded to the ligand-binding domain of FXR.[1]
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00499629 Healthy Phase 1 Completed - United States, Pennsylvania ... 展开 >> Facility Philadelphia, Pennsylvania, United States, 19148 收起 <<
NCT00509756 Healthy Phase 1 Terminated(Please see terminat... 展开 >>ion statement in the detailed description.) 收起 << - Japan ... 展开 >> Tokyo, Japan, 171-0014 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.28mL

0.46mL

0.23mL

11.40mL

2.28mL

1.14mL

22.81mL

4.56mL

2.28mL
参考文献

[1]Flatt B, et al. Discovery of XL335 (WAY-362450), a highly potent, selective, and orally active agonist of the farnesoid X receptor (FXR). J Med Chem. 2009 Feb 26;52(4):904-7.

[2]Evans MJ, et al. A synthetic farnesoid X receptor (FXR) agonist promotes cholesterol lowering in models of dyslipidemia. Am J Physiol Gastrointest Liver Physiol. 2009 Mar;296(3):G543-52.

[3]Hartman HB, et al. Activation of farnesoid X receptor prevents atherosclerotic lesion formation in LDLR-/- and apoE-/- mice. J Lipid Res. 2009 Jun;50(6):1090-100.