VU 0424465

Catalog # Availability Size / Price Qty
6895/10
6895/50
Group I mGluR Modulators Small Molecule
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Description: Potent mGlu5 positive allosteric modulator and agonist; binds allosteric site with high affinity

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

Purity: ≥98%

Product Details
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Biological Activity

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.

Technical Data

M.Wt:
326.37
Formula:
C19H19FN2O2
Solubility:
Soluble to 100 mM in DMSO and to 100 mM in ethanol
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
1428630-85-6

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

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