产品
编 号:F205024
分子式:C18H19BrClFN2O
分子量:413.71
产品类型
结构图
CAS No: 1706524-94-8
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产品详情
生物活性:
ML-00253764 hydrochloride is a brain penetrant nonpeptidic melanocortin receptor 4 (MC4R) antagonist with a Ki and IC50 of 0.16 μM and 0.103 μM, respectively.
体内研究:
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 (For?reference?only).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.
体外研究:
ML-00253764 displaces NDP-α-MSH binding with a mean IC50 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.