INT-767

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Chemical Structure| 1000403-03-1 同义名 : -
CAS号 : 1000403-03-1
货号 : A405369
分子式 : C25H43NaO6S
纯度 : 98%
分子量 : 494.66
MDL号 : -
存储条件:

Pure form

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(212.27 mM),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

H2O: 100 mg/mL(202.16 mM),配合低频超声助溶

动物实验配方:
生物活性
描述 INT-767 is a potent agonist for both FXR (mean EC50, 30 nM by PerkinElmer AlphaScreen assay) and TGR5 (mean EC50, 630 nM by time resolved-fluorescence resonance energy transfer).
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.02mL

0.40mL

0.20mL

10.11mL

2.02mL

1.01mL

20.22mL

4.04mL

2.02mL

参考文献

[1]Baghdasaryan A, Claudel T,et al. Dual farnesoid X receptor/TGR5 agonist INT-767 reduces liver injury in the Mdr2-/- (Abcb4-/-) mouse cholangiopathy model by promoting biliary HCO⁻₃ output. Hepatology. 2011 Oct;54(4):1303-12.

[2]Rizzo G, Passeri D, et al. Functional characterization of the semisynthetic bile acid derivative INT-767, a dual farnesoid X receptor and TGR5 agonist. Mol Pharmacol. 2010 Oct;78(4):617-30.