Devazepide
(Synonyms: 地伐西匹; L-364,718; MK-329) 目录号 : GC18139
Devazepide (L-364,718) 是一种有效、竞争性、选择性和口服活性的胆囊收缩素 (CCK) 受体非肽拮抗剂，对大鼠胰腺、牛胆囊和豚鼠脑 CCK 受体的 IC50 分别为 81 pM、45 pM 和 245 nM .
Cas No.:103420-77-5
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
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]
References:
[1] Dickenson, John M. , and Stephen J. Hill. "Synergistic interactions between human transfected adenosine A 1 receptors and endogenous cholecystokinin receptors in CHO cells."?European journal of pharmacology?302.1 (1996): 141-151.
[2] Lavigne, G. J., W. R. Millington, and G. P. Mueller. "The CCK-A and CCK-B receptor antagonists, devazepide and L-365,260, enhance morphine antinociception only in non-acclimated rats exposed to a novel environment."Neuropeptides?21.2 (1992): 119-129.
[3] Pu, Su-Fen, Hui-Xin Zhuang, and Ji-Sheng Han. "Cholecystokinin octapeptide (CCK-8) antagonizes morphine analgesia in nucleus accumbens of the rat via the CCK-B receptor."?Brain research?657.1 (1994): 159-164.
[4] D'amato, M. , I. F. Stamford, and A. Bennett. "Studies of three non‐peptide cholecystokinin antagonists (devazepide, lorglumide and loxiglumide) in human isolated alimentary muscle and guinea‐pig ileum."?British journal of pharmacology?102.2 (1991): 391-395.
| Cas No. | 103420-77-5 | SDF | |
| 别名 | 地伐西匹; L-364,718; MK-329 | ||
| 化学名 | (S)-N-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-1H-indole-2-carboxamide | ||
| Canonical SMILES | O=C1N(C)C2=CC=CC=C2C(C3=CC=CC=C3)=N[C@@H]1NC(C4=CC5=CC=CC=C5N4)=O | ||
| 分子式 | C25H20N4O2 | 分子量 | 408.46 |
| 溶解度 | <40.85mg/ml in DMSO; <20.42mg/ml in ethanol | 储存条件 | Store at -20°C, sealed storage, away from moisture and light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.4482 mL | 12.2411 mL | 24.4822 mL |
| 5 mM | 0.4896 mL | 2.4482 mL | 4.8964 mL |
| 10 mM | 0.2448 mL | 1.2241 mL | 2.4482 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet