KAT681
KAT681 is a liver-selective thyromimetic.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 373641-87-3
- 分子式: C24H21FNNaO6
- 分子量:461.41
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
Thyroid Hormone Receptor[1]
体外実験
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[1]
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 373641-87-3
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分子量 461.41
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分子式 C24H21FNNaO6
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SMILES
O=C(CC(NC1=CC(C)=C(C(C)=C1)OC2=CC=C(C(C(O)C3=CC=C(C=C3)F)=C2)O)=O)O[Na]
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別名
T0681
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
Cell Assay[2]
HepG2 cells are used. At a confluency of 70%, HepG2 cells are incubated with 50 μg/mL of acetylated LDL (AcLDL) for 24 h and subsequently treated with indicated amounts of KAT681 (0.5 μM) in serum-free medium for another 24 h. Cellular protein extraction and Western blot analysis are performed.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Rabbits[1]
Male NZW rabbits are subcutaneously implanted with Alzet osmotic pumps carrying KAT681 (36 nmoles/kg/day) in 1% DMSO/PBS or 1% DMSO/PBS alone as control for the entire duration of the studies. Rabbits are fed a 0.2% cholesterol and 3.5% fat diet or a 2% cholesterol and 5% fat diet. Food consumption is restricted to 100 g/day/animal. At the end of the studies, animals are fasted 5 h before the collection of blood samples, killed by a threefold overdose of pentobarbital, and organ biopsies snap-frozen.
Mice[2]
Male C57/B6 (WT) mice are fed a standard chow diet. After 2 weeks of acclimatization, mice are divided into two groups and subcutaneously implanted with Alzet micro-osmotic pumps carrying KAT681 in PBS (36 nmol/kg/d) or PBS alone as control for 14 days. After 14 days of treatment, animals are fasted for 5 h and anesthetized. Blood samples are taken, mice sacrificed by cervical dislocation, and organ biopsies are snap-frozen. Male SR-BI KO and LDLr KO mice are fed a standard chow diet, and subcutaneously implanted with Alzet micro-osmotic pumps carrying KAT681 in PBS (36 nmol/kg/d) or PBS alone as control. Mice are then fasted for 5 h, blood samples are taken, mice are sacrificed by cervical dislocation, and liver biopsies are snap-frozen.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
参考文献
[1]. Tancevski I, et al. The thyromimetic T-0681 protects from atherosclerosis. J Lipid Res. 2009 May;50(5):938-44. [Content Brief]
[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. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)