Tetrahydromagnolol
(Synonyms: 二丙基联苯二醇,Magnolignan) 目录号 : GC15327
An agonist of CB1 and CB2 and antagonist of GPR55
Cas No.:20601-85-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Tetrahydromagnolol is a major metabolite of magnolol and acts as a peripheral CB2 receptor agonist. Tetrahydromagnolol also acts as an antagonist at GPR55 [1].
Cannabinoid (CB) receptors belong to the G protein-coupled receptor (GPCR) superfamily and are divided into CB1 and CB2. CB1 activation mediates analgesia, stimulation of appetite, and euphoria, among other effects. CB2 receptor activation results in analgesic and antiinflammatory effects. GPR55, a CB-related orphan receptor, is reported to interact with certain CBs [1].
Tetrahydromagnolol is a highly selective peripheral CB2 receptor agonist that is 19-fold more potent than magnolol with EC50 and Ki values of 0.17 μM and 0.42 μM, respectively. Magnolol is a bioactive compound isolated from the bark of Magnolia officinalis that is used in Asian traditional medicine for the treatment of anxiety, sleeping disorders, and allergic diseases. Magnolol behaved as a partial agonist with selectivity for the CB2 subtype (EC50 = 3.28 μM; Ki = 1.44 μM). In β-arrestin translocation assay, Tetrahydromagnolol inhibited LPI-induced GPR55 activation with KB value of 13.3 μM [1].
Reference:
[1]. Rempel V, Fuchs A, Hinz S, et al. Magnolia Extract, Magnolol, and Metabolites: Activation of Cannabinoid CB2 Receptors and Blockade of the Related GPR55. ACS Med Chem Lett. 2012 Nov 14;4(1):41-5.
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.6982 mL | 18.4911 mL | 36.9822 mL |
| 5 mM | 0.7396 mL | 3.6982 mL | 7.3964 mL |
| 10 mM | 0.3698 mL | 1.8491 mL | 3.6982 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。
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