AVE-1625
(Synonyms: 屈那班,Drinabant) 目录号 : GC14115
A potent CB1 receptor antagonist
Cas No.:358970-97-5
Sample solution is provided at 25 µL, 10mM.
AVE-1625 is a highly potent, selective antagonist for the CB1 receptor [1].
The cannabinoid receptor type 1 (CB1) is a G protein-coupled receptor mainly expressed in the central and peripheral nervous system. The CB1 receptor is activated by the endocannabinoid neurotransmitters anandamide and 2-arachidonoylglycerol (2-AG). The CB1 receptor has been implicated in the maintenance of homeostasis in health and disease [2]. The CB1 receptor plays vital roles in modulating neurotransmitter release by preventing the development of excessive neuronal activity, reducing pain and other inflammatory symptoms [2].
AVE-1625 antagonized the CB1 receptor activity with the Ki values of 0.16-0.44 nM [1]. Treatment with AVE-1625 (1-3 mg/kg) significantly improved the performance of rodents in working memory tasks. At 30 mg/kg, AVE-1625 reduced caloric intake by more than 50% of controls and significantly increased lipolysis from fat tissues and reduced hepatic glycogen levels in rodents. In Wistar rats, postprandially administration of AVE1625 slightly increased the basal lipolysis in a dose-dependent manner. AVE1625 caused primary effects on metabolic blood and tissue parameters as well as metabolic rate [3]. As measured by indirect calorimetry, AVE1625 immediately increased the total energy expenditure and a transiently increased glucose oxidation [3].
References:
[1] Borowsky B, Stevens R, Mark B, et al. AVE1625, a cannabinoid CBI antagonist, as a co-treatment for schizophrenia: Improvement in cognitive function and reduction of antipsychotic-side effects in animal models[C]//Neuropsychopharmacology. Macmillan building, 4 crinan st, london n1 9xw, ENGLAND: NATURE PUBLISHING GROUP, 2005, 30: S116-S117.
[2] Herkenham M, Lynn A B, Little M D, et al. Cannabinoid receptor localization in brain[J]. Proceedings of the national Academy of sciences, 1990, 87(5): 1932-1936.
[3] Herling A W, Gossel M, Haschke G, et al. CB1 receptor antagonist AVE1625 affects primarily metabolic parameters independently of reduced food intake in Wistar rats[J]. American Journal of Physiology-Endocrinology and Metabolism, 2007, 293(3): E826-E832.
Cas No. | 358970-97-5 | SDF | |
别名 | 屈那班,Drinabant | ||
化学名 | N-[1-[bis(4-chlorophenyl)methyl]azetidin-3-yl]-N-(3,5-difluorophenyl)methanesulfonamide | ||
Canonical SMILES | CS(=O)(N(C1CN(C(C2=CC=C(Cl)C=C2)C3=CC=C(Cl)C=C3)C1)C4=CC(F)=CC(F)=C4)=O | ||
分子式 | C23H20Cl2F2N2O2S | 分子量 | 497.4 |
溶解度 | ≤0.15mg/ml in ethanol;15mg/ml in DMSO;15mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
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。 |
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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。 |
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1 mg | 5 mg | 10 mg |
1 mM | 2.0105 mL | 10.0523 mL | 20.1045 mL |
5 mM | 0.4021 mL | 2.0105 mL | 4.0209 mL |
10 mM | 0.201 mL | 1.0052 mL | 2.0105 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
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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