KAT681 - CAS 373641-87-3
Category: Inhibitor
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KAT681 is a novel liver-selective thyromimetic displaying strong hypolipidemic properties without cardio-toxic effects.
T 0681; T-0681; T0681; Propanoic acid, 3-​[[4-​[3-​[(4-​fluorophenyl)​hydroxymethyl]​-​4-​hydroxyphenoxy]​-​3,​5-​dimethylphenyl]​amino]​-​3-​oxo-​, sodium salt (1:1)
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1.Inhibitory effects of KAT-681, a liver-selective thyromimetic, on development of hepatocellular proliferative lesions in rats induced by 2-acetylaminofluorene and partial hepatectomy after diethylnitrosamine initiation.
Hayashi M;Ohnota H;Tamura T;Kuroda J;Shibata N;Akahane M;Moriwaki H;Machida N;Mitsumori K Arch Toxicol. 2004 Aug;78(8):460-6. Epub 2004 Mar 19.
To examine the potential inhibitory effects of a novel liver-selective thyromimetic, KAT-681 (KAT), on the development of hepatocellular proliferative lesions, male F344 rats were given a single intraperitoneal injection of 150 mg/kg diethylnitrosamine (DEN), followed by gavage administration of 7.5 mg/kg per day of 2-acetylaminofluorene (2-AAF) twice daily from weeks 2 to 4 with partial hepatectomy (PH) at week 3. From 5 weeks after the completion of 2-AAF administration, the rats were orally dosed with 0.04, 0.1, or 0.25 mg/kg per day KAT for 3 weeks, and subjected to morphometric analysis of the induced glutathione S-transferase placental form (GST-P)-positive lesions and hepatocellular adenomas (HCAs). Administration of KAT significantly and dose-dependently reduced the total area of GST-P-positive lesions (by 34-48%) and also their numbers (by 20-44%), their mean size not being significantly changed. No effects on the number of HCAs were apparent, although a reduction in their mean size was detected at a dose of 0.25 mg/kg per day KAT (by 34%). On biochemical analysis, serum activity of gamma-glutamyl transpeptidase, an enzyme related to hepatocarcinogenesis, was markedly reduced in rats given 0.
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CAS 373641-87-3 KAT681

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