MB-07811

MB-07811 is a liver-targeted prodrug form of the thyroid hormone receptor β (TRβ) agonist MB-07344.¹ It is stable in extrahepatic tissues and converted to MB-07344 in the liver. MB-07811 binds to TRα1 and TRβ1 with K_i values of 12.5 and 14.6 µM, respectively. Oral administration of MB-07811 reduces plasma cholesterol levels (ED₅₀ = 0.48 mg/kg) in a cholesterol-fed rat (CFR) model. It also reduces hepatic steatosis, as well as plasma levels of cholesterol, in Zucker diabetic fatty rats in a model of non-alcoholic fatty liver disease (NAFLD) when administered at a dose of 5 mg/kg per day.² MB-07811 (10 mg/kg) reverses hepatic steatosis, reducing total hepatic lipids without decreasing body weight, in a mouse model of diet-induced obesity.

WARNING This product is not for human or veterinary use.

1. Boyer, S.H., Jiang, H., Jacintho, J.D., et al. Synthesis and biological evaluation of a series of liver-selective phosphonic acid thyroid hormone receptor agonists and their prodrugs. J. Med. Chem. 51(22), 7075-7093 (2008).

2. Cable, E.E., Finn, P.D., Stebbins, J.W., et al. Reduction of hepatic steatosis in rats and mice after treatment with a liver-targeted thyroid hormone receptor agonist. Hepatology 49(2), 407-417 (2009).