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

Chemical Structure : Devazepide

CAS No.: 103420-77-5

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Devazepide (L-364,718, MK-329)

货号: PC-22021Not For Human Use, Lab Use Only.

Devazepide (L-364,718) is a potent, competitive, selective and orally active nonpeptide antagonist of peripheral cholecystokinin (CCK) receptor with IC50 of 81 pM, 45 pM and 245 nM for rat pancreatic, bovine gallbladder and guinea pig brain CCK receptors.

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5 mg ￥1380 In stock
10 mg ￥2180 In stock
25 mg ￥3780 In stock
50 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

Devazepide (L-364,718) is a potent, competitive, selective and orally active nonpeptide antagonist of peripheral cholecystokinin (CCK) receptor with IC50 of 81 pM, 45 pM and 245 nM for rat pancreatic, bovine gallbladder and guinea pig brain CCK receptors.
Devazepide is a competitive CCK antagonist, which lacks agonist activity.
Devazepide exhibits a very high selectivity for peripheral CCK receptors relative to brain CCK, gastrin, and various other peptide and nonpeptide receptors in both in vitro radioligand and isolated tissue assays.
Devazepide (0.1 mg/kg) markedly antagonized the contractions of the guinea pig gallbladder produced by intravenous administration of CCK for at least 2 hr.
Devazepide (ED50, 0.04 mg/kg, oral) is highly effective as an antagonist of CCK-induced inhibition of gastric emptying in mice.

物理化学性质&存储条件

分子量 408.46
分子式 C25H20N4O2
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

(S)-N-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-1H-indole-2-carboxamide

参考文献

1. Chang RS, et al. Proc Natl Acad Sci U S A. 1986 Jul;83(13):4923-6.

2. Chang RS, et al. Mol Pharmacol. 1986 Sep;30(3):212-7.

3. Lotti VJ, et al. J Pharmacol Exp Ther. 1987 Apr;241(1):103-9.

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