GPR88 agonist 2
GPR88 agonist 2（化合物53）是一种强效的脑渗透型GPR88激动剂，在GPR88-cAMP功能测定中的EC50值为14μM。
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包装价格促销价数量
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1mg￥1987.001590.00- +
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5mg￥4812.003850.00- +
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10mg￥7700.006160.00- +
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- 货号: ajcf26842
- CAS: 2821859-71-4
- 别名:
- 分子式: C26H33N5O3
- 分子量: 463.57
- 纯度: ＞98%
- 溶解度: DMSO : 100 mg/mL (215.72 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
- 储存: -20°C
- 库存: 现货
Background
GPR88 agonist 2 (compound 53) is a potent and brain-penetrantGPR88 agonist with an EC50 value of 14 μM in GPR88 cAMP functional assay.GPR88 agonist 2 significantly enhance [35S]GTPγS binding activity (EC50: 8.9 μM) in WT mouse striatal membranes, but GPR88 agonist 2 is inactive in striatal membranes prepared from GPR88 KO mice.[1].
GPR88 agonist 2 (20mg/ml, ip) has a good plasma exposure (Cmax:1670 ng/mL) and acceptable metabolic stability (T1/2:4.66h, CL:21mL/mg/kg)[1].
GPR88 agonist 2 (20mg/ml, ip) has sufficient brain penetration (Cmax:576 ng/mL)[1].
Pharmacokinetic analysis in mice[1]
| 20 mg/kg, ip | Cmax (ng/mL) | T1/2 (h) | CL(mL/min/kg) | B/Pratio |
| plasma | 1670 | 5.6 | 21 | 0.34 |
| brain | 576 | / | / |
