您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > ML-00253764 hydrochloride
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
ML-00253764 hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
ML-00253764 hydrochloride图片
CAS NO:1706524-94-8
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
ML-00253764 是一种非肽类黑皮质素受体 4 (MC4R) 拮抗剂,其KiIC50值分别为 0.16 μM 和 0.103 μM。脑渗透剂。
生物活性

ML-00253764 hydrochloride is a brain penetrant nonpeptidicmelanocortin receptor4 (MC4R)antagonist with aKiandIC50of 0.16 μM and 0.103 μM, respectively[1].

IC50& Target

Ki: 0.16 μM
IC50: 0.103 μM (melanocortin receptor 4)[1]

体外研究
(In Vitro)

ML-00253764 displaces NDP-α-MSH binding with a mean IC50of 0.32 μM, 0.81 μM and 2.12 μM for hMC4-R, hMC3-R and hMC5-R, respectively[1].
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[1].

体内研究
(In Vivo)

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[1].
ML-00253764 dissolves in polyethylene glycol 200/saline (1:10) in a volume of 10 mL/kg (For reference only)[1].

Animal Model:CT-26 tumor bearing BALB/c mice[1]
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.
分子量

413.71

Formula

C18H19BrClFN2O

CAS 号

1706524-94-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.