MB-07811 (VK-2809) is an orally active HepDirect prodrug of MB07344, a liver-targeted thyroid hormone receptor-β agonist. MB-07811 has cholesterol and triglycerides lowering activity.
MB-07811 (VK-2809) 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].
MB-07811 (VK-2809) (0.3-30 mg/kg; orally once daily for 14 days) reduces cholesterol and triglycerides in diet-induced obese mice[2].
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.