ML-00253764 hydrochloride
目录号: PL07069 纯度: ≥98%
CAS No. :1706524-94-8
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中文名称
ML-00253764 hydrochloride
中文别名
化合物 T12072
英文名称
ML-00253764 hydrochloride
英文别名
2-[2-[2-(5-Bromo-2-methoxyphenyl)ethyl]-3-fluorophenyl]-4,5-dihydro-2-1H-imidazole hydrochloride;ML-00253764 hydrochloride
Cas No.
1706524-94-8
分子式
C18H19BrClFN2O
分子量
413.71
包装储存
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
产品详情
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。
生物活性
ML-00253764 hydrochloride is a brain penetrant nonpeptidic melanocortin receptor 4 (MC4R) antagonist with a K i and IC 50 of 0.16 μM and 0.103 μM, respectively.
性状
Solid
IC50 & Target[1][2]
Ki: 0.16 μM
IC50: 0.103 μM (melanocortin receptor 4)
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.
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.
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.
ML-00253764 dissolves in polyethylene glycol 200/saline (1:10) in a volume of 10 mL/kg (For reference only). has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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 Me
溶解度数据
In Vitro: DMSO : 12.5 mg/mL (30.21 mM; ultrasonic and warming and heat to 60°C)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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