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Vipadenant

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Chemical Structure| 442908-10-3 同义名 : BIIB-014;CEB-4520;VER-ADO-49;VER-A00049;VER-A00-11;VER-11135;V-2006
CAS号 : 442908-10-3
货号 : A155723
分子式 : C16H15N7O
纯度 : 99%+
分子量 : 321.337
MDL号 : MFCD12024697
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(93.36 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Vipadenant is a selective Adenosine A2A receptor with Ki value of 1.3nM. It exhibits much lower affinity to A1 and A2B with Ki value of 63nM, and Ki value of 1005nM for A3. Vipadenant had a minimum effective dose of 0.1 and 1 mg/kg in the mouse and rat haloperidol-induced hypolocomotion models in vivo, respectively. Vipadenant was able to increase contralateral rotations in 6-OHDA lesioned rats when dosed orally in combination with apomorphine at 3 and 10 mg/kg. Vipadenant also showed reversal of motor disability in MPTP-treated marmosets without dyskinesias at a minimum effective dose of <5 mg/kg, p.o.[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.11mL

0.62mL

0.31mL

15.56mL

3.11mL

1.56mL

31.12mL

6.22mL

3.11mL
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.