ML-00253764 HYDROCHLORIDE
| 中文名称 | ML-00253764 HYDROCHLORIDE |
|---|---|
| 中文同义词 | 化合物 T12072 |
| 英文名称 | ML-00253764 (hydrochloride) |
| 英文同义词 | 2-[2-[2-(5-Bromo-2-methoxyphenyl)ethyl]-3-fluorophenyl]-4,5-dihydro-2-1H-imidazole hydrochloride;ML00253764 hydrochloride,ML 00253764 hydrochloride |
| CAS号 | 1706524-94-8 |
| 分子式 | C18H19BrClFN2O |
| 分子量 | 413.72 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 1706524-94-8.mol |
| 结构式 |  |
ML-00253764 HYDROCHLORIDE 性质
| 储存条件 | Store at -20°C |
|---|---|
| 溶解度 | DMF：30mg/mL； DMF:PBS (pH 7.2) (1:20)：0.5mg/mL；二甲基亚砜：25mg/mL；乙醇：1mg/mL |
| 形态 | 结晶固体 |
| 颜色 | 米白色至浅黄色 |
ML-00253764 是一种非肽类黑皮质素受体4 (MC4R) 拮抗剂，其 Ki 和 IC50 值分别为 0.16 µM 和 0.103 µM。脑渗透剂。
ML-00253764 displaces NDP-α-MSH binding with a mean IC 50 of 0.32 μM, 0.81 μM and 2.12 μM for hMC4-R, hMC3-R and hMC5-R, respectively. ML-00253764 (100 µM) decreases cAMP production induced by [NLE4,D-Phe7]-α-melanocyte stimulating hormone ([NDP]-α-MSH) by 20% in MC4R-expressing HEK293 cell membranes, but has no effect on cAMP levels in MC3R- or MC5R-expressing membranes.
ML-00253764 (subcutaneous injection; 3, 10, or 30 mg/kg; once daily) shows protection against tumor-induced body weight loss upon chronic, peripheral dosing in CT-26 tumor bearing BALB/c mice.ML-00253764 dissolves in polyethylene glycol 200/saline (1:10) in a volume of 10 ml/kg.
| Animal Model: | CT-26 tumor bearing BALB/c mice |
| Dosage: | 3, 10, or 30 mg/kg |
| Administration: | Subcutaneous injection; 3, 10, or 30 mg/kg; once daily |
| Result: | Reduced tumor-induced weight loss in a mouse model. |