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首页-小分子抑制剂&激动剂-GPCR-Melanocortin Receptor-ML00253764 hydrochloride
ML00253764 hydrochloride

Chemical Structure : ML00253764 hydrochloride

CAS No.: 1706524-94-8

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ML00253764 hydrochloride (ML 00253764)

货号: PC-61574Not For Human Use, Lab Use Only.

ML00253764 hydrochloride is a non-peptide, brain penetrant melanocortin MC4 receptor (MC4R) antagonist with IC50 of 0.32, 0.81 and 2.12 uM for MC4, MC3 and MC5 receptors, respectively.

规格 价格 库存 数量
5 mg ￥1380 In stock
10 mg ￥2180 In stock
25 mg ￥3580 In stock
50 mg Get quote
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

ML00253764 hydrochloride is a non-peptide, brain penetrant melanocortin MC4 receptor (MC4R) antagonist with IC50 of 0.32, 0.81 and 2.12 uM for MC4, MC3 and MC5 receptors, respectively.
ML00253764 decreases cAMP accumulation in HEK-293 cells expressing the MC4 receptor, increases food intake and effectively reduces tumor-induced weight loss in mouse model.
ML00253764 exhibits an antiproliferative and proapoptotic activity through the inhibition of the phosphorylation of ERK1/2 and Akt in glioblastoma cell, also shows highly synergistic effect combined with temozolomide both in vitro and in vivo.

物理化学性质&存储条件

分子量 413.71
分子式 C18H18BrFN2O.HCl
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

2-[2-[2-(5-bromo-2- methoxyphenyl)-ethyl]-3-fluorophenyl]-4,5-dihydro-1H-imidazole hydrochloride

参考文献

1. Vos TJ, et al. J Med Chem. 2004 Mar 25;47(7):1602-4.

2. Nicholson JR, et al. J Pharmacol Exp Ther. 2006 May;317(2):771-7.

3. Vaglini F, et al. Mol Neurobiol. 2017 Aug 8. doi: 10.1007/s12035-017-0702-4.

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