VU 0424465

Key Product Details

Product Description

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 (K_i = 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 G_s in HEK 293 cells. Induces epileptiform activity in CA3 hippocampal neurons in vitro and convulsions in vivo.

Product Specifications for VU 0424465

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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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

Calculators

Background References

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

• Sengmany Biased allosteric agonism and modulation of metabotropic glutamate receptor 5: Implications for optimizing preclinical neuroscience drug discovery. Neuropharmacology 2017 PMID: 27392634
• Nasrallah Direct coupling of detergent purified human mGlu₅ receptor to the heterotrimeric G proteins Gq and Gs. Sci.Rep. 2018 PMID: 29535347
• Rook Unique signaling profiles of positive allosteric modulators of metabotropic glutamate receptor subtype 5 determine differences in in vivo activity. Biol.Psychiatry. 2013 PMID: 23140665

Product Documents for VU 0424465