CAS No.: 442908-10-3
Vipadenant Catalog No. CSN18277
Synonyms: BIIB-014;CEB-4520;V2006
Vipadenant is an adenosine antagonist with Ki of 1.3 nM and 68 nM for A2A and A1, respectively. Vipadenant is a selective A2A receptor antagonist with Ki values of 1.3, 68, 63, and 1,005 nM for A2A, A1, A2B, and A3 receptors, respectively, used in development for for Parkinson's disease.
| 规格 | 价格 | 促销价格 | 库存 | 数量 |
|---|
400-920-2911
sales@csnpharm.cn
tech@csnpharm.cn
纯度 & 质量文件
批次:
靶点选择性
生物活性
靶点 Adenosine Receptor A2A
Ki:1.3nMAdenosine Receptor A1
Ki:68nM- 描述
动物研究 剂量 Rat: 2 mg/kg, 5 mg/kg[2] (p.o.); 1 mg/kg, 2 mg/kg[2] (i.v.); 0.3 mg/kg - 30 mg/kg[3] (i.p.)
给药途径 p.o., i.v., i.p.
动物药代数据 Animal Rats[2] Dose 2 mg/kg Administration p.o. or i.v. F 30.4 ± 8.9% T1/2 65.2 ± 20.2 min (p.o.)
71.2 ± 8.5 min (i.v.)Tmax 7.5 ± 5.0 min (p.o.)
2.0 ± 0.0 min (i.v.)AUClast 16716.4 ± 7245.0 min·ng/ml (p.o.)
90694.2 ± 18814.6 min·ng/ml (i.v.)CL 22.5 ± 4.3 ml/min/kg (i.v.) Cmax 229.7 ± 88.0 min (p.o.)
3091.0 ± 221.6 min (i.v.)Vss 1209.3 ± 174.4 ml/kg (i.v.) - 参考文献
- [1] Adenosine A2A Receptor Antagonists and Parkinson’s Disease
- [2] Shin SH, Park MH, et al. Analysis of Vipadenant and Its In Vitro and In Vivo Metabolites via Liquid Chromatography-Quadrupole-Time-of-Flight Mass Spectrometry. Pharmaceutics. 2018 Dec 3;10(4). pii: E260.
- [3] Jones N, Bleickardt C, 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.
实验方案
- 计算器
- 储存液制备
技术信息
| CAS号 | 442908-10-3 | 储存条件 |
|
|||
| 分子式 | C16H15N7O | 运输 | 蓝冰 | |||
| 分子量 | 321.34 | 别名 | BIIB-014;CEB-4520;V2006;VER-11135;VER-A00-11;VER-A00049;VER-ADO-49 | |||
| 溶解度 |
|
动物实验配方 |
