SNT-207858 free base 是一种选择性，能透过血脑屏障的，有口服活性的黑皮质素 (melanocortin; MC-4) 受体拮抗剂，SNT-207858 free base 抑制与 MC-4 受体结合，IC50 为 22 nM。SNT-207858 抑制 MC-4 活性，IC50 为 11 nM。
货号:ajcx14326
CAS:1104662-66-9
分子式:C32H43Cl2N5O3
分子量：616.62
溶解度:DMSO: 125 mg/mL (202.72 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

SNT207858 free base is a selective, blood brain barrier penetrating, potent and orally active melanocortin-4 (MC-4) receptor antagonist. SNT207858 free base has an IC50 of 22 nM (binding) and 11 nM (function) on the MC-4 receptor[1].

SNT207858 binds to the MC-4 receptor with an affinity of 22 nM and shows a 170-fold selectivity vs. MC-3 and a 40-fold selectivity vs. MC-5[1].

SNT207858 (30 mg/kg; oral administration; once daily; 15 days) significantly reduces the tumor induced weight loss in mice[1]. Animal Model: Mice with C26 adenocarcinoma-induced cachexia model[1]

[1]. Weyermann P, et al. Orally available selective melanocortin-4 receptor antagonists stimulate food intake and reduce cancer-induced cachexia in mice. PLoS One. 2009;4(3):e4774.