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

Chemical Structure : Antalarmin

CAS No.: 157284-96-3

Antalarmin

货号: PC-23838Not For Human Use, Lab Use Only.

Antalarmin is a potent, selective nonpeptide corticotropin-releasing factor receptor 1 (CRHR1, CRF1) antagonist with Ki of 2.7 nM, with no effect on CRF2 receptor.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Antalarmin is a potent, selective nonpeptide corticotropin-releasing factor receptor 1 (CRHR1, CRF1) antagonist with Ki of 2.7 nM, with no effect on CRF2 receptor.
Antalarmin potently displaced 125I-oCRH binding, exhibiting respectively Ki values of 1. 9 nM, 1.3 nM, and 1.4 nM in pituitary, cerebellum, and frontal cortex ho- mogenates.
Antalarmnin (20 mg/kg body wt.) significantly inhibited CRH-stimulated ACTH release and carageenin-induced subcutaneous inflammation in rats.

物理化学性质&存储条件

分子量 378.56
分子式 C24H34N4
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

N-Butyl-N-ethyl-7-mesityl-2,5,6-trimethyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine

参考文献

1. Deak T, et al. Endocrinology. 1999 Jan;140(1):79-86.

2. Webster EL, et al. Endocrinology. 1996 Dec;137(12):5747-50.

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