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首页-小分子抑制剂&激动剂-GPCR-Melanocortin Receptor-CRN04894
CRN04894

Chemical Structure : CRN04894

CAS No.: 2392970-97-5

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CRN04894 (CRN-04894, CRN 04894)

货号: PC-38702Not For Human Use, Lab Use Only.

CRN04894 is a highly potent, selective, orally available melanocortin 2 receptor (MC2R antagonist) antagonist with Ki of 2.1 nM.

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10 mg ￥5980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

CRN04894 is a highly potent, selective, orally available melanocortin 2 receptor (MC2R antagonist) antagonist with Ki of 2.1 nM.
CRN04894 selectively blocks the ACTH-MC2R interaction, showing no binding to MC1R, MC3R, MC4R, and MC5R at concentrations >1 uM.
CRN04894 demonstrates remarkable efficacy in a rat model of adrenocorticotrophic hormone (ACTH)-stimulated corticosterone secretion.
Oral administration of CRN04894 suppressed ACTH-stimulated corticosterone secretion in a dose-dependent manner at doses ≥3 mg/kg. 

物理化学性质&存储条件

分子量 613.73
分子式 C33H42F3N5O3
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

6-(2-ethoxyphenyl)-3-((R)-2-ethyl-4-(1-(trifluoromethyl)cyclobutane-1-carbonyl)piperazin-1-yl)-N-((S)-quinuclidin-3-yl)picolinamide

参考文献

1. Kim SH, et al. ACS Med Chem Lett. 2024 Mar 19;15(4):478-485.

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