化合物 T15644 T15644

Product Introduction
Bioactivity


英文名: KAT681

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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

关键字: KAT 681 | T 0681 | T-0681 | KAT-681 | KAT681

相关产品: Sobetirome | REVERSE T3 | PCO371 | TR antagonist 1 | DS08210767 | NH-3 | Resmetirom | Carbimazole | Protirelin | 3,5-Diiodothyropropionic acid

化合物 T15644 T15644信息由TargetMol中国为您提供，如您想了解更多关于化合物 T15644 T15644报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途