MB-07811

Names

[ Name ]:
MB-07811

Biological Activity

[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.

Chemical & Physical Properties

[ Density]:
1.27±0.1 g/cm3(Predicted)

[ Boiling Point ]:
660.6±55.0 °C(Predicted)

[ Melting Point ]:
77-82 °C

[ Molecular Formula ]:
C₂₈H₃₂ClO₅P

[ Molecular Weight ]:
514.98

[ Exact Mass ]:
514.16800

[ PSA ]:
74.80000

[ LogP ]:
8.08420

[ Storage condition ]:
2-8°C

MB-07811

Names

Biological Activity

Chemical & Physical Properties

Related Compounds