VU6005649

SKU: orb1308946

Description

VU6005649 is a centrally penetrant small molecule agonist for the mGlu7 and mGlu8 receptors, exhibiting EC50 values of 0.65 µM and 2.6 µM, respectively. This compound is a valuable research tool for investigating the role of these receptors in neurological and psychiatric disorders, supporting both in vitro binding studies and in vivo behavioral experiments.

Research Area

Neuroscience

Key Properties

• CAS Number: 2137047-43-7
• MW: 357.28
• Purity: 99.79%
• Formula: C₁₆H₁₂F₅N₃O
• SMILES: COc1ccc(-c2c(C)nn3c(cc(C)nc23)C(F)(F)F)c(F)c1F
• Target: GluR
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.6 mM);DMSO:60 mg/mL (167.94 mM)

Bioactivity

• Target IC50:
  mGluR7:0.65 μM (EC50)|mGluR8:2.6 μM
• In Vivo:
  In wild-type mice VU6005649 shows modest but significant pro-cognitive effects on associative learning and the first example of efficacy of an mGlu7/8 positive allosteric modulator (PAM) in this model.
• In Vitro:
  VU6005649 is an agonist of CNS penetrant mGlu7/8 receptor(EC50s of 0.65 μM and 2.6 μM for mGlu7 receptor and mGlu8 receptor, respectively). VU6005649 displays a terminal Kp of 2.43 with total brain levels ~9× above the mGlu7 positive allosteric modulator (PAM) in vitro EC50.

Storage & Handling

• Storage: 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

inhibit, Metabotropic glutamate receptors, mGlu7, mGlu7 receptor, mGlu8, mGlu8 receptor, mGluR, Inhibitor, VU 6005649, VU6005649, VU-6005649

Compound Identifiers

PubChem CID

131954513