Monoacylglycerol Lipase Inhibitor 21
(Synonyms: MAGL Inhibitor 21,MGL Inhibitor 21) 目录号 : GC12031
A reversible blocker of 2-AG hydrolysis
Cas No.:1643657-35-5
Sample solution is provided at 25 µL, 10mM.
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Ki: 0.4 μM for MAGL
Monoacylglycerol Lipase Inhibitor 21 is an inhibitor of monoacylglycerol lipase (MAGL) and FAAH.
Endocannabinoids such as 2-arachidonoyl glycerol (2-AG) and arachidonoyl ethanolamide (AEA) are biologically active lipids involved in various synaptic processes including activation of cannabinoid receptors. Fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL) mediate the hydrolysis of AEA and 2-AG, respectively.
In vitro: A previous study confirmed that Monoacylglycerol Lipase Inhibitor 21 could inhibit MAGL in a reversible manner. Moreover, the kinetic studies indicated that Monoacylglycerol Lipase Inhibitor 21 acted as a noncompetitive inhibitor. In addition, Monoacylglycerol Lipase Inhibitor 21 did not bind CB1 or CB2 receptors. Furthermore, the selectivity of Monoacylglycerol Lipase Inhibitor 21 was studied in a broad panel that includes a variety of receptors and enzymes, and the results showed that Monoacylglycerol Lipase Inhibitor 21 did not inhibit significantly any of the analyzed targets [1].
In vivo: Multiple sclerosis (MS) mouse model was used to evaluated the in-vivo efficacy of Monoacylglycerol Lipase Inhibitor 21. Treatment started at day 6 post-immunization and consisted of daily injections of Monoacylglycerol Lipase Inhibitor 21 (5 mg/kg, i.p.) for the following 21 days. Results showed that the administration of Monoacylglycerol Lipase Inhibitor 21 could clearly ameliorate the progression of the disease, as assessed by the significantly lower clinical score in the MS model. This improvement correlated with an increase of the 2-AG levels in the spinal cord of treated animalsand with evident changes at the histological level, as Monoacylglycerol Lipase Inhibitor 21 was able to significantly decrease leukocyte infiltration and microglial response, prevent axonal damage, as well as partially restore myelin morphology in EAE mice [1].
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Hernández-Torres, G. ,Cipriano, M.,Hedén, E., et al. A reversible and selective inhibitor of monoacylglycerol lipase ameliorates multiple sclerosis. Angewandte Chemistry International Edition English 53(50), 13765-13770 (2014).
| Cas No. | 1643657-35-5 | SDF | |
| 别名 | MAGL Inhibitor 21,MGL Inhibitor 21 | ||
| 化学名 | 1,3-benzodioxol-5-ylmethyl ester [1,1'-biphenyl]-4-hexanoic acid | ||
| Canonical SMILES | O=C(OCC1=CC(OCO2)=C2C=C1)CCCCCC(C=C3)=CC=C3C4=CC=CC=C4 | ||
| 分子式 | C26H26O4 | 分子量 | 402.5 |
| 溶解度 | ≤21mg/ml in ethanol;0.5mg/ml in DMSO;30mg/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 | 2.4845 mL | 12.4224 mL | 24.8447 mL |
| 5 mM | 0.4969 mL | 2.4845 mL | 4.9689 mL |
| 10 mM | 0.2484 mL | 1.2422 mL | 2.4845 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