Vipadenant

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效且选择性的 A2A 腺苷受体，Ki 为 1.3 nM。

A potent and selective A2A adenosine receptor with Ki of 1.3 nM; displays 50-fold selectivity over A1 and A2B, and no activity against A3, P450 isoforms and hERG; shows excellent preclinical pharmacokinetics, and demonstrates strong oral activity in commonly used models of Parkinson's disease.(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. 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.

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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.

BIIB-014 | BIIB 014 | BIIB014

Apoptosis

Adenosine Receptor

A1|A2A|A3

Neurological Disease

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442908-10-3

321.3366

C16H15N7O

>98% (HPLC)

DMSO: ≥ 31 mg/mL

NC1=NC(C2=CC=CO2)=C(N=NN3CC4=CC=C(N)C(C)=C4)C3=N1

3H-1,2,3-Triazolo[4,5-d]pyrimidin-5-amine, 3-[(4-amino-3-methylphenyl)methyl]-7-(2-furanyl)-

(-20℃)

With Ice Pack

≥ 2 years