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。
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.
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