KAT681 (T0681)

Catalog No. Size PriceQuantity
M22371-C Contact sales@xcessbio.com for quotation $100Unavailable


KAT681 is a liver-selective thyromimetic. The impact of the liver-selective thyromimetic KAT681 (T-0681) is investigated on lipoprotein metabolism. Prolonged treatment with KAT681 increases the hepatic expression of both low-density lipoprotein (LDL) receptor and scavenger receptor class B, type I without affecting cholesteryl ester transfer protein activity. 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. SR-BI protein expression is markedly downregulated by incubation with 50 μg/mL AcLDL. This effect can not be reversed by addition of KAT681 In preliminary dose-titration studies, a marked decrease of plasma cholesterol is observed at 36 nmoles/kg/day KAT681 (T-0681), whereas doses higher than 36 nmoles/kg/day show no further lipid-lowering effect. In the subsequent study, New Zealand White (NZW) rabbits are fed a 0.2% cholesterol diet and dosed with 36 nmoles/kg/day KAT681 or a respective placebo control for 4 weeks. KAT681 treatment results in a 60% decrease of plasma cholesterol and a 70% decrease of plasma triglycerides. In preliminary dose-titration studies in wild-type (WT) mice, 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. Higher doses than 36 nmol/kg/d show no further lipid-lowering effect. KAT681 significantly increases hepatic LDLrs in SR-BI KO mice (2-fold of controls, P<0.01), along with a marked decrease in plasma cholesterol. . Tancevski I, et al. The thyromimetic T-0681 protects from atherosclerosis. J Lipid Res. 2009 May;50(5):938-44. . 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.

Product information

CAS Number: 373641-87-3

Molecular Weight: 462.42

Formula: C24H22FNNaO6

Chemical Name: 2-[(4-{3-[(4-fluorophenyl)(hydroxy)methyl]-4-hydroxyphenoxy}-3,5-dimethylphenyl)carbamoyl]acetic acid sodium

Smiles: [Na].CC1C=C(C=C(C)C=1OC1C=C(C(O)C2C=CC(F)=CC=2)C(O)=CC=1)NC(=O)CC(O)=O |^1:0|


InChi: InChI=1S/C24H22FNO6.Na/c1-13-9-17(26-21(28)12-22(29)30)10-14(2)24(13)32-18-7-8-20(27)19(11-18)23(31)15-3-5-16(25)6-4-15;/h3-11,23,27,31H,12H2,1-2H3,(H,26,28)(H,29,30);

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.

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