| 产品描述: | CB1/2 agonist 1 is a potent and cross the blood-brain barrier CB1/2 agonist with EC50s of 56.15, 11.63 nM for CB1R and CB2R, respectively. CB1/2 agonist 1 reduces glutamate release and LPS-induced activation of microglial cells. CB1/2 agonist 1 shows anti-inflammatory and antinociceptive effects. CB1/2 agonist 1 has the potential for the research of multiple sclerosis. |
| 靶点: |
hCB1-R:56.15 nM (EC50); cannabinoid type-2 receptors:11.63 nM (EC50) |
| 体外研究: |
CB1/2 agonist 1 (5-50 mg/kg) dose-dependently relieves neuropathic pain in a mouse model of oxaliplatin-induced neuropathic pain. |
| 体内研究: |
CB1/2 agonist 1 (compound B2) (10 µM) inhibits AEA hydrolysis with an IC50 of 5.9 µM for FAAH. CB1/2 agonist 1 shows high affinity for CB1R and CB2R with Kis of 2.9, 1.5 nM, respectively. CB1/2 agonist 1 (10 µM) shows anti-inflammatory effect and significantly decreases the secretion of IL-1β and IL-6, increases the release of anti-inflammatory IL-10 to 483.7% in LPS-activated BV-2 cells. CB1/2 agonist 1 (1, 10 µM) inhibits 4-AP-evoked glutamate release. |
| 参考文献: |
1. Arena C, et al. The endocannabinoid system dual-target ligand N-cycloheptyl-1,2-dihydro-5-bromo-1-(4-fluorobenzyl)-6-methyl-2-oxo-pyridine-3-carboxamide improves disease severity in a mouse model of multiple sclerosis. Eur J Med Chem. 2020 Dec 15;208:112858. |
| 保存条件: |
-80°C 6个月;-20°C 1个月 |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.297 ml |
11.486 ml |
22.971 ml |
| 5 mM |
0.459 ml |
2.297 ml |
4.594 ml |
| 10 mM |
0.23 ml |
1.149 ml |
2.297 ml |
| 50 mM |
0.046 ml |
0.23 ml |
0.459 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |