ML-00253764 hydrochloride

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CAS NO:

1706524-94-8

ML-00253764 是一种非肽类黑皮质素受体 4 (MC4R) 拮抗剂，其K_i和IC₅₀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 aK_iandIC₅₀of 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.