MK-0493

Names

[ CAS No. ]:
455956-93-1

[ Name ]:
MK-0493

Biological Activity

[Description]:

MK-0493 is a potent, orally active and selective agonist of the melanocortin receptor 4 (MC4R), demonstrating significant reductions in energy intake[1].

[Related Catalog]:

Research Areas >> Endocrinology
Research Areas >> Metabolic Disease
Signaling Pathways >> GPCR/G Protein >> Melanocortin Receptor

[In Vivo]

MK-0493 dose-dependently increases electrically evoked increases in ICP[2]. MK-0493 is shown to promote robust weight loss activity following oral administration in preclinical animal models, suggesting the drug can access the target site in the hypothalamus[3].

[References]

[1]. Krishna R, etal. Potent and selective agonism of the melanocortin receptor 4 with MK-0493 does not induce weight loss in obese human subjects: energy intake predicts lack of weight loss efficacy. Clin Pharmacol Ther. 2009 Dec;86(6):659-66.

[2]. Sezen SF, et al. Intracavernosal pressure monitoring in mice: responses to electrical stimulation of the cavernous nerve and to intracavernosal drug administration. J Androl. 2000 Mar-Apr;21(2):311-5.

[3]. Hong Q, et al. Discovery of a piperazine urea based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist. Bioorg Med Chem Lett. 2011 Apr 15;21(8):2330-4.

Chemical & Physical Properties

[ Molecular Formula ]:
C30H38ClF2N3O2

[ Molecular Weight ]:
546.09

Related Compounds