包装: | 5mg |
规格: | 98% |
市场价: | 9525元 |
分子量: | 546.09 |
Background:
MK-0493 is a potent, orally active and selective agonist of the melanocortin receptor 4 (MC4R), demonstrating significant reductions in energy intake[1].
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].
[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.