Dipraglurant

SKU: orb1707374

Description

Dipraglurant (ADX48621) is a selective mGluR5 negative allosteric modulator. It has demonstrated efficacy in reducing levodopa-induced dyskinesia (LID) in primate models, supporting its research application in Parkinson's disease and related movement disorders.

Research Area

Neuroscience

Key Properties

• CAS Number: 872363-17-2
• MW: 265.29
• Purity: 98.70% (May vary between batches)
• Formula: C₁₆H₁₂FN₃
• SMILES: Fc1ccc2nc(CCC#Cc3ccccn3)cn2c1
• Target: GluR
• Solubility: DMSO:40 mg/mL (150.78 mM)

Bioactivity

• Target IC50:
  mGluR5:21 nM
• In Vivo:
  Dipraglurant (3-30 mg/kg; single oral dose) exhibits favorable pharmacokinetics and reduces levodopa-induced dyskinesia and muscle tone disturbances without interfering with the efficacy of levodopa treatment in parkinsonian disabled monkeys .
• In Vitro:
  The novel mGlu receptor negative allosteric modulator (NAM) bifunctional agent Dipraglurant(1-10 μM; 15 minutes) counteracted the abnormal membrane responses and calcium elevations induced by the D2R agonist quinpirole or (NPEC-dopamine) in both models.

Storage & Handling

• Storage: store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Dipraglurant, ADX 48621, ADX48621, ADX-48621, mGluR5

Compound Identifiers

PubChem CID

44557636