1104662-66-9
中文名稱
SNT-207858 free base
英文名稱
SNT-207858 free base
CAS
1104662-66-9
分子式
C32H43Cl2N5O3
分子量
616.62
MOL 文件
1104662-66-9.mol
1104662-66-9 結(jié)構(gòu)式
基本信息
中文別名
化合物 T12945 英文別名
SNT-207858 free base1-Pyrrolidinecarboxamide, N-[(1R)-1-[(2,4-dichlorophenyl)methyl]-2-oxo-2-[4-[3-[(2R)-2-(1-pyrrolidinyl)butoxy]-2-pyridinyl]-1-piperidinyl]ethyl]-
物理化學(xué)性質(zhì)
沸點(diǎn)813.0±65.0 °C(Predicted)
密度1.258±0.06 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMSO: 125 mg/mL (202.72 mM)
酸度系數(shù)(pKa)12.71±0.20(Predicted)
形態(tài)Solid
顏色White to off-white
常見問題列表
生物活性
SNT-207858 free base 是一種選擇性，能透過血腦屏障的，有口服活性的黑皮質(zhì)素 (melanocortin; MC-4) 受體拮抗劑，SNT-207858 free base 抑制與 MC-4 受體結(jié)合，IC50 為 22 nM。SNT-207858 抑制 MC-4 活性，IC50 為 11 nM。靶點(diǎn)
MC-4 receptor
體外研究
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.
體內(nèi)研究
SNT207858 (30 mg/kg; oral administration; once daily; 15 days) significantly reduces the tumor induced weight loss in mice.
| Animal Model: | Mice with C26 adenocarcinoma-induced cachexia model |
| Dosage: | 30 mg/kg |
| Administration: | Oral administration; once daily; 15 days |
| Result: | Significantly reduced the tumor induced weight loss. |