MB-07811

MB-07811 is a liver-targeted prodrug form of the thyroid hormone receptor beta (TRbeta) agonist MB-07344. It is stable in extrahepatic tissues and converted to MB-07344 in the liver. MB-07811 binds to TRalpha1 and TRbeta1 with Ki 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. MB-07811 (10 mg/kg) reverses hepatic steatosis, reducing total hepatic lipids without decreasing body weight, in a mouse model of diet-induced obesity.Formal Name: 4-[[4-[[(2R,4S)-4-(3-chlorophenyl)-2-oxido-1,3,2-dioxaphosphorinan-2-yl]methoxy]-2,6-dimethylphenyl]methyl]-2-(1-methylethyl)-phenol. CAS Number: 852948-13-1. Synonyms: VK-2809. Molecular Formula: C28H32ClO5P. Formula Weight: 515.0. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: Acetonitrile: Soluble, DMSO: Soluble. SMILES: OC1=C(C(C)C)C=C(C=C1)CC2=C(C=C(C=C2C)OC[P@]3(OCC[C@H](O3)C4=CC=CC(Cl)=C4)=O)C. InChi Code: InChI=1S/C28H32ClO5P/c1-18(2)25-14-21(8-9-27(25)30)15-26-19(3)12-24(13-20(26)4)32-17-35(31)33-11-10-28(34-35)22-6-5-7-23(29)16-22/h5-9,12-14,16,18,28,30H,10-11,15,17H2,1-4H3/t28-,35+/m0/s1. InChi Key: LGGPZDRLTDGYSQ-JADSYQMUSA-N.