Vipadenant

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Vipadenant

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:	442908-10-3
规格:	≥98%

包装与价格：

包装	价格(元)
5mg	询价
10mg	询价
25mg	询价
50mg	询价
100mg	询价
250mg	询价
500mg	询价

理化性质和储存条件

Molecular Weight (MW)	321.34
Formula	C16H15N7O
CAS No.	442908-10-3
Storage	-20℃ for 3 years in powder form
Storage	-80℃ for 2 years in solvent
Solubility (In vitro)	DMSO: ≥ 30 mg/mL
	Water: N/A
	Ethanol: N/A
Chemical Name	3-(4-amino-3-methylbenzyl)-7-(furan-2-yl)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-5-amine
Synonyms	CEB-4520; VER-11135; CEB4520; BIIB014; BIIB 014;V-2006; VER-A00-11; VER-A00049; CEB 4520; BIIB-014; V2006; V 2006; VER-ADO-49
SMILES Code	NC1=NC(C2=CC=CO2)=C(N=NN3CC4=CC=C(N)C(C)=C4)C3=N1

实验参考方法

Target	Ki: 1.3 nM (A2A), 68 nM (A1)[1], 1005 nM (A3)[2]
In Vivo	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[1]. 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[2].
References	[1]. A2A receptor antagonists do not induce dyskinesias in drug-naive or L-dopa sensitized rats. Brain Res Bull. 2013 Sep;98:163-9. [2]. Adenosine A2A Receptor Antagonists and Parkinson’s Disease. ACS Chem Neurosci. 2011 Oct 19; 2(10): 555-567

Target

Ki: 1.3 nM (A2A), 68 nM (A1)[1], 1005 nM (A3)[2]

In Vivo

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[1]. 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[2].

References

[1]. A2A receptor antagonists do not induce dyskinesias in drug-naive or L-dopa sensitized rats. Brain Res Bull. 2013 Sep;98:163-9.

[2]. Adenosine A2A Receptor Antagonists and Parkinson’s Disease. ACS Chem Neurosci. 2011 Oct 19; 2(10): 555-567