NESS 0327
目录号 : GC18041
A potent CB1 receptor antagonist
Cas No.:494844-07-4
Sample solution is provided at 25 µL, 10mM.
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Ki: 0.35 pM and 21 nM for CB1 and CB2 receptor, respectively.
NESS 0327 is an extremely potent cannabinoid (CB) receptor antagonist.
Cannabinoid CB1 receptors are present in the central nervous system with the highest densities in the hippocampus, and to a lesser extent in some peripheral tissues. Cannabinoid CB2 receptors are predominantly located in peripheral tissues. Both receptors can negatively regulate adenylate cyclase and control the release of arachidonic acid.
In vitro: Previous study found that NESS 0327 exhibited a stronger selectivity for CB1 receptor compared with SR 141716A, showing a much higher affinity for CB1 receptor and a higher affinity for the CB2 receptor. Affinity ratios demonstrated that NESS 0327 was more than 60,000-fold selective for the CB1 receptor. NESS 0327 alone did not produce concentration-dependent stimulation of guanosine 5'-O-(3-[35S]thio)-triphosphate binding in rat cerebella membranes. Conversely, NESS 0327 antagonized WIN 55,212-2-stimulated guanosine 5'-O-(3-[35S]thio)-triphosphate binding. In functional assay, NESS 0327 could antagonize the inhibitory effects of WIN 55,212-2 on electrically evoked contractions in mouse isolated vas deferens preparations [1].
In vivo: In vivo studies showed that NESS 0327 could antagonize the antinociceptive effect produced by WIN 55,212-2 in both tail-flick and hot-plate test, suggesting that NESS 0327 was a novel cannabinoid antagonist with high selectivity for the cannabinoid CB1 receptor [1].
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Ruiu, S. ,Pinna, G.A.,Marchese, G., et al. Synthesis and characterization of NESS 0327: A novel putative antagonist of the CB1 cannabinoid receptor. Journal of Pharmacology and Experimental Therapeutics 306(1), 363-370 (2003).
| Cas No. | 494844-07-4 | SDF | |
| 化学名 | 8-chloro-1-(2,4-dichlorophenyl)-1,4,5,6-tetrahydro-N-1-piperidinyl-benzo[6,7]cyclohepta[1,2-c]pyrazole-3-carboxamide | ||
| Canonical SMILES | Clc1ccc2c(CCCc3c(nn(c23)c2ccc(Cl)cc2Cl)C(=O)NN2CCCCC2)c1 | ||
| 分子式 | C24H23Cl3N4O | 分子量 | 489.8 |
| 溶解度 | ≤0.25mg/ml in ethanol;0.25mg/ml in DMSO;0.5mg/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。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0416 mL | 10.2082 mL | 20.4165 mL |
| 5 mM | 0.4083 mL | 2.0416 mL | 4.0833 mL |
| 10 mM | 0.2042 mL | 1.0208 mL | 2.0416 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet