ML-00253764 hydrochloride

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ML-00253764 hydrochloride 

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 hydrochloride

ML-00253764 hydrochloride Chemical Structure

CAS No. : 1706524-94-8

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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[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 IC50 of 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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.
参考文献

  • [1]. Vos TJ, et al. Identification of 2-[2-[2-(5-bromo-2- methoxyphenyl)-ethyl]-3-fluorophenyl]-4,5-dihydro-1H-imidazole (ML00253764), a small molecule melanocortin 4 receptor antagonist that effectively reduces tumor-induced weight loss in a mouse model. J Med Chem. 2004 Mar 25;47(7):1602-4.

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