VU 0424465

Pricing Availability   Qty
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% (HPLC)
Literature (6)

Biological Activity for VU 0424465

VU 0424465 is a 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 for VU 0424465

M. Wt 326.37
Formula C19H19FN2O2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1428630-85-6
PubChem ID 53384864
Smiles C[C@H](C(C)(O)C)NC(C1=CC=C(C#CC2=CC(F)=CC=C2)C=N1)=O

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.

Solubility Data for VU 0424465

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 32.64 100
ethanol 32.64 100

Preparing Stock Solutions for VU 0424465

The following data is based on the product molecular weight 326.37. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.06 mL 15.32 mL 30.64 mL
5 mM 0.61 mL 3.06 mL 6.13 mL
10 mM 0.31 mL 1.53 mL 3.06 mL
50 mM 0.06 mL 0.31 mL 0.61 mL

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References for VU 0424465

References are publications that support the biological activity of the product.

Rook et al (2013) Unique signaling profiles of positive allosteric modulators of metabotropic glutamate receptor subtype 5 determine differences in in vivo activity. Biol.Psychiatry. 73 501 PMID: 23140665

Sengmany et al (2017) Biased allosteric agonism and modulation of metabotropic glutamate receptor 5: Implications for optimizing preclinical neuroscience drug discovery. Neuropharmacology 115 60 PMID: 27392634

Nasrallah et al (2018) Direct coupling of detergent purified human mGlu5 receptor to the heterotrimeric G proteins Gq and Gs. Sci.Rep. 8 4407 PMID: 29535347

If you know of a relevant reference for VU 0424465, please let us know.

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Citations for VU 0424465

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Metabotropic Glutamate Receptors Scientific Review

Metabotropic Glutamate Receptors Scientific Review

Written by Francine Acher, this review discusses the pharmacology and therapeutic potential of mGlu receptors, and the compounds acting upon them; compounds available from Tocris are listed.

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