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• 产品描述： INT-767 is a dual farnesoid X receptor (FXR)/TGR5 agonist with mean EC50s of 30 and 630 nM, respectively

• 靶点： FXR;G protein-coupled Bile Acid Receptor 1;Autophagy;FXR; GPCR19

• 体外研究：
  INT-767 does not show cytotoxic effects in HepG2 cells, does not inhibit cytochrome P450 enzymes, is highly stable to phase I and II enzymatic modifications, and does not inhibit the human ether-a-go-go-related gene potassium channel

• 体内研究：
  INT-767 (10-20 mg/kg; i.p.; daily for 2 weeks) decreases plasma total cholesterol and triglyceride levels in db/m and db/db mice. Animal Model: Male 8-week old C57BKS/J db/db mice, control nondiabetic db/m mice Dosage: 10, 20 mg/kg Administration: Intraperitoneal injection; daily for 2 weeks Result: Decreased plasma total cholesterol and triglyceride levels.

• 参考文献：
  1. Baghdasaryan A, et al. Dual farnesoid X receptor/TGR5 agonist INT-767 reduces liver injury in the Mdr2-/- (Abcb4-/-) mousecholangiopathy model by promoting biliary HCO3- output. Hepatology. 2011 Oct;54(4):1303-1312. 2. Rizzo G, et al. Functional characterization of the semisynthetic bile acid derivative INT-767, a dual farnesoid X receptor andTGR5 agonist. Mol Pharmacol. 2010 Oct;78(4):617-630.

• 溶解性： soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.022 ml	10.108 ml	20.216 ml
  5 mM	0.404 ml	2.022 ml	4.043 ml
  10 mM	0.202 ml	1.011 ml	2.022 ml
  50 mM	0.04 ml	0.202 ml	0.404 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *