852948-13-1

852948-13-1 structure

Name: MB-07811
Chemical Name: 4-[[4-[[(2R,4S)-4-(3-chlorophenyl)-2-oxo-1,3,2λ5-dioxaphosphinan-2-yl]methoxy]-2,6-dimethylphenyl]methyl]-2-propan-2-ylphenol
CAS Number: 852948-13-1
Molecular Formula: C₂₈H₃₂ClO₅P
Molecular Weight: 514.98
Catalog: Research Areas Metabolic Disease
Create Date: 2017-08-14 20:12:25
Modify Date: 2024-01-08 16:34:15
MB-07811 (VK-2809) is an orally active HepDirect prodrug of MB07344, a liver-targeted thyroid hormone receptor-β agonist[1]. MB-07811 has cholesterol and triglycerides lowering activity[2].

Name	4-[[4-[[(2R,4S)-4-(3-chlorophenyl)-2-oxo-1,3,2λ5-dioxaphosphinan-2-yl]methoxy]-2,6-dimethylphenyl]methyl]-2-propan-2-ylphenol

Description	MB-07811 (VK-2809) is an orally active HepDirect prodrug of MB07344, a liver-targeted thyroid hormone receptor-β agonist[1]. MB-07811 has cholesterol and triglycerides lowering activity[2].
Related Catalog	Signaling Pathways >> Others >> Thyroid Hormone Receptor Research Areas >> Metabolic Disease
Target	Thyroid hormone receptor-β[2]
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].
In Vivo	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.
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.