Vipadenant

SKU: orb1305579

Description

Vipadenant (CEB-4520, BIIB-014) is a potent and selective adenosine A2a receptor antagonist with a Ki of 1.3 nM, demonstrating 53-fold selectivity over the A1 receptor (Ki=69 nM). This compound is a valuable research tool for investigating adenosine signaling in neurological disorders, with applications in both in vitro binding assays and in vivo Parkinson's disease models.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 442908-10-3
• MW: 321.34
• Purity: 98.00% (May vary between batches)
• Formula: C₁₆H₁₅N₇O
• SMILES: Cc1cc(Cn2nnc3c(nc(N)nc23)-c2ccco2)ccc1N
• Target: Adenosine Receptor
• Solubility: DMSO:55 mg/mL (171.16 mM)

Bioactivity

• Target IC50:
  A2A:1.3 nM(Ki)|A1:69 nM(Ki)
• In Vivo:
  Vipadenant, administered at doses ranging from 0.3 to 30 mg/kg, effectively reduces catalepsy in a dose-dependent manner without inducing statistically significant dyskinetic episodes in 6-OHDA-lesioned rats at a dosage of 10 mg/kg through a 19-day treatment protocol. Moreover, in models of haloperidol-induced hypolocomotion in mice and rats, the minimum effective doses of vipadenant are 0.1 mg/kg and 1 mg/kg, respectively. Additionally, oral administration of vipadenant at 3 and 10 mg/kg is shown to increase contralateral rotations in 6-OHDA lesioned rats, indicating its potential in modulating motor functions.
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Storage & Handling

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

Alternative Names

inhibit, Inhibitor, CEB 4520, CEB4520, CEB-4520, A1, A3, A2A, Adenosine Receptor, AdenosineReceptor, BIIB 014, BIIB014, BIIB-014, P1 receptor, Vipadenant

Compound Identifiers

PubChem CID

21874557