GSK360A

Names

[ Name ]:
GSK360A

[Synonym ]:
gsk360a

Biological Activity

[Description]:

GSK360A is a potent and orally active HIF-PHD inhibitor with IC50 values of 10, 100, and 126 nM for PHD1, PHD2, and PHD3, respectively. GSK360A activates the HIF-1 alpha pathway and protect the failing heart after myocardial infarction (MI) [1].

[Related Catalog]:

Research Areas >> Cardiovascular Disease

Signaling Pathways >> Metabolic Enzyme/Protease >> HIF/HIF Prolyl-Hydroxylase

[In Vivo]

GSK360A (30 mg/kg i.g.) 在已建立的心室功能障碍模型中改善长期心室功能、重塑和血管分布[1]。 Animal Model: male Lewis rats with ventricular dysfunction model[1] Dosage: 30 mg/kg Administration: oral gavage Result: Increased circulating levels of erythropoietin and hemoglobin and hemoxygenase-1 expression in the heart and skeletal muscle of male rats.

[References]

[1]. Bao W, et, al. Chronic inhibition of hypoxia-inducible factor prolyl 4-hydroxylase improves ventricular performance, remodeling, and vascularity after myocardial infarction in the rat. J Cardiovasc Pharmacol. 2010 Aug;56(2):147-55.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₇H₁₇FN₂O₅

[ Molecular Weight ]:
348.33

[ Exact Mass ]:
348.11200

[ PSA ]:
112.12000

[ LogP ]:
2.03550