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KAT681

Catalog No. T15644   CAS 373641-87-3
Synonyms: T0681

KAT681 is a liver selective thyromimetic.

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KAT681 Chemical Structure
KAT681, CAS 373641-87-3
Pack Size Availability Price/USD Quantity
25 mg 6-8 weeks $ 1,520.00
50 mg 6-8 weeks $ 1,980.00
100 mg 6-8 weeks $ 2,500.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description KAT681 is a liver selective thyromimetic.
In vitro 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].
In vivo 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.
Synonyms T0681
Molecular Weight 462.429
Formula C24H22FNNaO6
CAS No. 373641-87-3

Storage

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

TargetMolReferences and Literature

1. Tancevski I, et al. The thyromimetic T-0681 protects from atherosclerosis. J Lipid Res. 2009 May;50(5):938-44. 2. Tancevski I, et al. The liver-selective thyromimetic T-0681 influences reverse cholesterol transport and atherosclerosis development in mice. PLoS One. 2010 Jan 15;5(1):e8722.

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Keywords

KAT681 373641-87-3 Endocrinology/Hormones Thyroid hormone receptor(THR) KAT 681 T 0681 T-0681 KAT-681 T0681 inhibitor inhibit

 

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