Vipadenant

SKU: orb1225040

Description

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.

Key Properties

• CAS Number: 442908-10-3
• MW: 321.3366
• Purity: >98% (HPLC)
• Formula: C₁₆H₁₅N₇O
• SMILES: NC1=NC(C2=CC=CO2)=C(N=NN3CC4=CC=C(N)C(C)=C4)C3=N1
• Target: Adenosine Receptor
• Solubility: DMSO: ≥ 31 mg/mL

Bioactivity

• 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.
  Read more...

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BIIB-014 | BIIB 014 | BIIB014

Quick Database Links

Gene Symbol

Adenosine Receptor