MK-0493 是有效的、具有口服活性的、选择性的黑皮质激素受体4 (MC4R) 的激动剂，可明显减少食物摄入。
货号:ajcx37592
CAS:455956-93-1
分子式:C30H38ClF2N3O2
分子量：546.09
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

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.