S88863 |
Vipadenant (BIIB 014) |
源叶(MedMol) | 98% |
- 产品描述: Vipadenant (BIIB-014; CEB-4520) is an adenosine receptor antagonist, with Kis of 1.3 nM and 68 nM for A2A and A1, respectively
- 靶点: Ki: 1.3 nM (A2A), 68 nM (A1), 1005 nM (A3);AdenosineReceptor
- 体内研究:
Vipadenant (0.3-30 mg/kg) produces a dose-dependent reduction in catalepsy. Vipadenant (10 mg/kg) does not produce any statistically significant dyskinetic episodes in 6-OHDA-lesioned rats during a 19-day dosing regimen. In the mouse and rat haloperidol-induced hypolocomotion models, vipadenant has a minimum effective dose of 0.1 and 1 mg/kg, respectively. Vipadenant (3 and 10 mg/kg, p.o.) is able to increase contralateral rotations in 6-OHDA lesioned rats
- 参考文献:
1. Jones N, et al. A2A receptor antagonists do not induce dyskinesias in drug-naive or L-dopa sensitized rats. Brain Res Bull. 2013 Sep;98:163-9. 2. Brian C. Shook, et al. Adenosine A2A Receptor Antagonists and Parkinson’s Disease. ACS Chem Neurosci. 2011 Oct 19; 2(10): 555-567.
- 溶解性: Soluble in DMSO
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 3.112 ml 15.56 ml 31.12 ml 5 mM 0.622 ml 3.112 ml 6.224 ml 10 mM 0.311 ml 1.556 ml 3.112 ml 50 mM 0.062 ml 0.311 ml 0.622 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)