Powder: -20°C for 3 years | In solvent: -80°C for 1 year
KAT681 is a liver selective thyromimetic.
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 10,600 | 6-8周 | ||
50 mg | ¥ 13,800 | 6-8周 | ||
100 mg | ¥ 17,500 | 6-8周 |
产品描述 | KAT681 is a liver selective thyromimetic. |
体外活性 | Prolonged treatment with KAT681 enhances the hepatic expression of both low-density lipoprotein (LDL) receptor and scavenger receptor class B, type I without affecting cholesteryl ester transfer protein activity. SR-BI protein expression is markedly downregulated by incubation with 50 μg/mL AcLDL. This effect can not be reversed by the addition of KAT681. Western blot showing human SR-BI (CLA-1) expression in normal HepG2 cells and in HepG2 cells loaded with AcLDL and subsequently incubated with vehicle or KAT681 [1]. |
体内活性 | KAT681 treatment causes a 60% decrease in plasma cholesterol and a 70% decrease in plasma triglycerides[1]. KAT681 obviously enhances hepatic LDLrs in SR-BI KO mice (2-fold of controls, P<0.01), along with a marked decrease in plasma cholesterol[2]. A marked decrease of plasma cholesterol is observed at 36 nmoles/kg/day KAT681 (T-0681), whereas doses higher than 36 nmoles/kg/day display no further lipid-lowering effect, in preliminary dose-titration studies. A marked increase of hepatic SR-BI expression at 36 nmol/kg/d KAT681 (T-0681) and a concomitant 50% decrease of plasma cholesterol are observed, in preliminary dose-titration studies in wild-type (WT) mice. New Zealand White (NZW) rabbits are fed a 0.2% cholesterol diet and dosed with 36 nmoles/kg/day KAT681 or respective placebo control for 4 weeks, in the subsequent study. Higher doses than 36 nmol/kg/d display no further lipid-lowering effect. |
别名 | T0681 |
分子量 | 462.429 |
分子式 | C24H22FNNaO6 |
CAS No. | 373641-87-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
KAT681 373641-87-3 Endocrinology/Hormones Thyroid hormone receptor(THR) KAT 681 T 0681 T-0681 KAT-681 T0681 Inhibitor inhibitor inhibit