7182960

Tocris Bioscience™ VU 0424465

Potent mGlu5 positive allosteric modulator and agonist; binds allosteric site with high affinity

Manufacturer: Fischer Scientific

CAS Number: 1428630-85-6

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Chemical Name or Material

5-[2-(2-(3-Fluorophenyl)ethynyl]-N-[(1R)-2-hydroxy-1,2-dimethylpropyl]-2-pyridinecarboxamide

CAS

1428630-85-6

Molecular Formula

C19H19FN2O2

Purity

98%

Other Options

Image Product Name Manufacturer Price Range
Tocris Bioscience™ VU 0424465
-- ₹ 23,848.44
Tocris Bioscience™ VU 0424465
-- ₹ 99,420.12

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Description

  • Potent mGlu5 positive allosteric modulator (EC50 = 1.5 nM) and agonist (EC50 = 171 nM; maximum effect is 65% that of glutamate)
  • Binds allosteric site with high affinity (Ki = 11.8 nM)
  • Increases maximum response to glutamate by 30%
  • Exhibits bias towards signaling via IP1 and ERK1/2 over iCa2+ in HEK293 and neuronal cells, and activates Gs in HEK 293 cells
  • Induces epileptiform activity in CA3 hippocampal neurons in vitro and convulsions in vivo .