GAT211
规格
| Cas Number | 102704-40-5(DMSO) |
| 规格或纯度 | 10mM in DMSO |
| 包装 | 1ml |
产品信息
| 品牌 | 阿拉丁 |
| 浓度 | 10mM in DMSO |
| 过滤标签 | Cannabinoid Receptor,GPCR/G Protein,神经元信号传导,Compound libraries |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 生化和生理学机理 | GAT211 是一种大麻素 1 受体（CB1R）正异位调节剂（PAM）。GAT211 可激活 cAMP 和 β-arrestin2，其 EC 50 值分别为 260 nM 和 650 nM。GAT211 可抑制神经病理性疼痛和/或炎症性疼痛。 |
| 英文描述 |
GAT211 is a cannabinoid 1 receptor (CB1R) positive allosteric modulator (PAM). GAT211 activates cAMP and β-arrestin2 with EC 50 values of 260 nM and 650 nM, respectively. GAT211 inhibits GAT211 can be used for neuropathic and/or inflammatory pain research In Vitro GAT211 is stable in both human- and rat-liver microsomal incubations, with t 1/2 of 28.4 min and 8.67 min, repsectively. GAT211 limits dopamine D2 receptor-mediated extracellular regulated kinase (ERK) phosphorylation in Neuro2a cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo GAT211 potentiates the inhibition of electrically evoked vas deferens contraction in the same system (EC 50 =11 nM, E max =70). GAT211 (0.3 mg/kg, 1 mg/kg, 3 mg/kg; 5 mL/kg; ip; 2 doses with 5 min interval) dose-dependently reduced locomotor activity and the acoustic startle response.GAT211 is dissolved in a vehicle of ethanol, kolliphor, and saline at a ratio of 1:1:6 and injected at a volume of 5 mL/kg. MCE has not independently confirmed the accuracy of these methods. They are for reference only. IC50& Target:CB1 |