N-((R)-3-(2,4-Dichlorophenyl)-1-oxo-1-(4-(3-((R)-2-(pyrrolidin-1-yl)butoxy)pyridin-2-yl)piperidin-1-yl)propan-2-yl)pyrrolidine-1-carboxamide;SNT-207858 (free base);SNT-207858 free base
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 IC 50 of 22 nM (binding) and 11 nM (function) on the MC-4 receptor.
性状
Solid
IC50 & Target[1][2]
MC-4 receptor
体外研究(In Vitro)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
SNT207858 (30 mg/kg; oral administration; once daily; 15 days) significantly reduces the tumor induced weight loss in mice. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: Mice with C
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[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.
溶解度数据
In Vitro: DMSO : 100 mg/mL (162.17 mM; Need ultrasonic)配制储备液