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首页-小分子抑制剂&激动剂-GPCR-CRF Receptor-BMK-C205
BMK-C205

Chemical Structure : BMK-C205

CAS No.: 2950971-22-7

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BMK-C205 (BMK-C 205)

货号: PC-21195Not For Human Use, Lab Use Only.

BMK-C205 (BMK-C 205) is a potent, selective corticotropin-releasing hormone receptor 1 (CRF1R) antagonist with IC50 of 74 nM in calcium mobilization assays, blocks hypothalamus-pituitary-adrenal (HPA) axis activation.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

BMK-C205 (BMK-C 205) is a potent, selective corticotropin-releasing hormone receptor 1 (CRF1R) antagonist with IC50 of 74 nM in calcium mobilization assays, blocks hypothalamus-pituitary-adrenal (HPA) axis activation.
BMK-C205 displays >100-fold selectivity over CRF2R.
BMK-C205 exhibits minimal inhibition against five major CYP450 isoforms at a concentration of 10  μM.
BMK-C205 (30 mg/kg, orally administered for 3 days) shows in vivo antidepressant response in mice, without causing hyperactivity, significantly decreases adrenocorticotropic hormone (ACTH) and corticosterone (CORT) levels in treated mice.

物理化学性质&存储条件

分子量 488.43
分子式 C23H30BrN5O2
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

8-(4-bromo-2,6-dimethoxyphenyl)-N-butyl-N-(cyclopropylmethyl)-2,7-dimethylpyrazolo[1,5-a][1,3,5]triazin-4-amine

参考文献

1. Hoyoung Kim, et al. Exp Mol Med. 2023 Sep 1. doi: 10.1038/s12276-023-01082-1.

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