VU 0357121

SKU: orb1222263

Description

VU0357121 is a positive allosteric modulator of mGlu5 receptors (EC50 = 33 nM). Mutagenesis studies indicate that VU0357121 and related analogues bind to a yet uncharacterized allosteric site on mGlu(5), distinct from CPPHA, yet share a functional interaction with the MPEP site.

Key Properties

• CAS Number: 433967-28-3
• MW: 305.32
• Purity: >98% (HPLC)
• Formula: C₁₇H₁₇F₂NO₂
• SMILES: CCCCOc1ccc(cc1)C(=O)Nc1c(cc(cc1)F)F
• Target: mGluR5
• Solubility: DMSO : ≥ 50 mg/mL; 163.76 mM

Bioactivity

• In Vitro:
  VU 0357121 has the ability to enhance glutamate sensitivity of mGlu5 is likely due to the interaction at a site on the receptor distinct from the MPEP binding site. VU 0357121 does not bind at the MPEP allosteric site of mGlu5, thus does not possess mGlu5 NAM activity. The A809V/rmGlu5 mutation inhibited the ability of VU 0357121 to shift the glutamate concentration response curve, whereas the response to VU 0357121 is not altered by the F585I/rmGlu5 mutation. VU 0357121 shows weaker cooperativity in the Ca2+ mobilization assay in the low-expressing HEK293A-mGlu5 cell line.

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

VU-0357121, VU0357121, VU 0357121

Quick Database Links

Gene Symbol

mGluR5