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Submit ReviewVU 0424465
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)
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 |
| InChI Key | ZPKZAFDYFVJULO-CYBMUJFWSA-N |
| 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 | |
|---|---|---|---|
| Solubility | |||
| 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.
| 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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Product Datasheets for VU 0424465
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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Keywords: VU 0424465, VU 0424465 supplier, VU0424465, metabotropic, glutamate, receptor, subtype, 5, mGlu5, mGluR, agonist, positive, allosteric, modulators, modulates, agonists, agonism, potent, high, affinity, Glutamate, (Metabotropic), Group, I, Receptors, 6895, Tocris Bioscience
Citations for VU 0424465
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