1706524-94-8
中文名稱
ML-00253764 HYDROCHLORIDE
英文名稱
ML-00253764 (hydrochloride)
CAS
1706524-94-8
分子式
C18H19BrClFN2O
分子量
413.72
MOL 文件
1706524-94-8.mol
1706524-94-8 結(jié)構(gòu)式
基本信息
中文別名
化合物 T12072 英文別名
2-[2-[2-(5-Bromo-2-methoxyphenyl)ethyl]-3-fluorophenyl]-4,5-dihydro-2-1H-imidazole hydrochloride物理化學性質(zhì)
儲存條件-20°C儲存
溶解度DMF: 30mg/mL; DMF:PBS (pH 7.2) (1:20): 0.5mg/mL; DMSO: 25mg/mL; Ethanol: 1mg/mL
形態(tài)結(jié)晶固體
顏色Off-white to light yellow
常見問題列表
生物活性
ML-00253764 是一種非肽類黑皮質(zhì)素受體4 (MC4R) 拮抗劑，其 Ki 和 IC50 值分別為 0.16 μM 和 0.103 μM。腦滲透劑。體外研究
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.
體內(nèi)研究
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. |