MB-07811 (0.3-30 mg/kg; orally once daily for 14 days) reduces cholesterol and triglycerides in diet-induced obese mice[2]. Animal Model: 4-week-old male C57BL/6 mice (diet-induced obese (DIO) mice)[2] Dosage: 0.3 mg/kg, 1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg Administration: Orally once daily; 14 days Result: Reduced total plasma cholesterol, and reduced plasma triglycerides (40%) at the highest doses.
In Vitro
MB-07811 is potential for liver targeting with a low affinity for thyroid hormone receptors (TRβ Ki = 14.6 ± 0.5 μM; TRα Ki = 12.5 ± 0.6 μM)[2].
Kinase Assay
Cell Assay
Animal Administration
References
[1]. Cable EE, et al. Reduction of hepatic steatosis in rats and mice after treatment with aliver-targeted thyroidhormone receptor agonist. Hepatology. 2009 Feb;49(2):407-17.
[2]. Erion MD, et al. Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index. Proc Natl Acad Sci U S A. 2007 Sep 25;104(39):15490-5.
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