產(chǎn)品目錄

規(guī)格	10mM (in 1mL DMSO) 5mg 10mg 25mg 50mg 100mg
CAS	103420-77-5
別名	N/A
化學(xué)名	(S)-N-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-1H-indole-2-carboxamide
分子式	C25H20N4O2
分子量	408.46
溶解度	<40.85mg/ml in DMSO; <20.42mg/ml in ethanol
儲(chǔ)存條件	Store at -20°C,
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

Devazepide is a potent CCK-A receptor antagonist with IC50 of 0.26 nM. [1]

Cholecystokinin (CCK) has long been recognized as the dominant regulator of gallbladder contraction. The cholecystokinetic activity of different fragments of CCK in human has been established in several studies both in vivo and in vitro. There are two subtypes of CCK receptor that were identified, CCK-A and CCK-B. CCK-A are mainly located in peripheral tissues but also found in brain, while CCK-B distribute throughout the rodent central nervous system.

Devazeptide inhibitory effect against sulphated C-terminal octapeptide of cholecystokinin (CCK-8) on total [3H] inositol phosphate accumulation in CHO-AI cells was investigated. The results revealed that devazepide possesses an inhibitory effect with IC50 of 0.26 ± 0.06 nM. CCK-8 is considered to be the most potent endogenous anti-opiate agent. Morphine analgesia could be antagonized by treatment of CCK-8. However, the effect of CCK-8 could be reversed by devazeptide which could also potentiate analgesia of morphine greatly at doses of 50ng and 200ng. [2, 3]

Devazepide is a benzodiazepine derivative that interacts competitively with rat pancreatic CCK receptors as determined by Scatchard analysis against the specific binding of 125I-labelled CCK. In guinea-pig isolated ileum and colon, devazepide competitively blocked CCK-induced contractions with a potency greatly exceeding that of other non-peptide CCK antagonists such as proglumide, dibutyryl cyclic GMP and benzotript. It is confirmed that devazepide is a highly potent CCK-OP antagonist in this tissue. [4]

特別提醒：

1. 本產(chǎn)品僅供科研使用。請(qǐng)勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請(qǐng)勿存放于普通住宅區(qū)。

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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