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首页-小分子抑制剂&激动剂-GPCR-Cholecystokinin Receptor-Netazepide
Netazepide

Chemical Structure : Netazepide

CAS No.: 155488-25-8

Netazepide (YF476;YF-476;Sograzepide)

货号: PC-60082Not For Human Use, Lab Use Only.

Netazepide (YF476, Sograzepide) is a potent, selective and orally active gastrin/CCK-2 antagonist with IC50 of 0.1 nM.

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

生物&药学活性

Netazepide (YF476, Sograzepide) is a potent, selective and orally active gastrin/CCK-2 antagonist with IC50 of 0.1 nM.
Netazepide (YF476, Sograzepide) displays >5,000-fold selectivity over CCK-1 receptors.
Netazepide (YF476, Sograzepide) inhibits pentagastrin-induced gastric acid secretion in anesthetized rats (ED50=87 nM/kg), and shows potential for the treatment of gastroesophageal reflux disease (GERD).
Netazepide (YF476, Sograzepide) also inhibits gastric neuroendocrine enterochromaffin-like (ECL) cell hyperplasia and gastric carcinoid tumor development.

物理化学性质&存储条件

分子量 498.587
分子式 C28H30N6O3
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

(R)-1-(1-(3,3-dimethyl-2-oxobutyl)-2-oxo-5-(pyridin-2-yl)-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-3-(3-(methylamino)phenyl)urea

参考文献

1. Semple G, et al. J Med Chem. 1997 Jan 31;40(3):331-41.

2. Takinami Y, et al. Aliment Pharmacol Ther. 1997 Feb;11(1):113-20.

3. Takemoto Y, et al. Arzneimittelforschung. 1998 Apr;48(4):403-7.

4. Kidd M, et al. Regul Pept. 2010 Jun 8;162(1-3):52-60.

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