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Submit ReviewVU 0360172 hydrochloride
Description: Positive allosteric modulator of mGlu5 receptors
Chemical Name: N-Cyclobutyl-6-[2-(3-fluorophenyl)ethynyl]-3-pyridinecarboxamide hydrochloride
Purity: ≥98% (HPLC)
Biological Activity for VU 0360172 hydrochloride
VU 0360172 hydrochloride is a positive allosteric modulator of mGlu5 receptors (EC50 = 16 nM; Ki = 195 nM). Selective for mGlu5; displays no significant activity at mGlu1, mGlu2 or mGlu4 receptors. Exhibits antipsychotic-like activity in a rodent model. Also reduces spontaneous spike and wave discharges without affecting motor behaviour in a rat model of absence epilepsy.
Compound Libraries for VU 0360172 hydrochloride
VU 0360172 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for VU 0360172 hydrochloride
| M. Wt | 330.78 |
| Formula | C18H15FN2O.HCl |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1309976-62-2 |
| PubChem ID | 53384852 |
| InChI Key | NBGAPTWZQXSEAA-UHFFFAOYSA-N |
| Smiles | FC1=CC=CC(C#CC2=CC=C(C(NC3CCC3)=O)C=N2)=C1.Cl |
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 0360172 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 16.54 | 50 | |
| ethanol | 8.27 | 25 |
Preparing Stock Solutions for VU 0360172 hydrochloride
The following data is based on the product molecular weight 330.78. 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 |
|---|---|---|---|
| 0.5 mM | 6.05 mL | 30.23 mL | 60.46 mL |
| 2.5 mM | 1.21 mL | 6.05 mL | 12.09 mL |
| 5 mM | 0.6 mL | 3.02 mL | 6.05 mL |
| 25 mM | 0.12 mL | 0.6 mL | 1.21 mL |
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Product Datasheets for VU 0360172 hydrochloride
References for VU 0360172 hydrochloride
References are publications that support the biological activity of the product.
Rodriguez et al (2010) Discovery of novel allosteric modulators of metabotropic glutamate receptor subtype 5 reveals chemical and functional diversity and in vivo activity in rat behavioral models of anxiolytic and antipsychotic activity. Mol.Pharmacol. 78 1105 PMID: 20923853
D'Amore et al (2013) Potentiation of mGlu5 receptors with the novel enhancer, VU0360172, reduces spontaneous absence seizures in WAG/Rij rats. Neuropharmacology 66 330 PMID: 22705340
If you know of a relevant reference for VU 0360172 hydrochloride, please let us know.
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Keywords: VU 0360172 hydrochloride, VU 0360172 hydrochloride supplier, VU0360172, hydrochloride, Positive, allosteric, modulators, mGlu5, mGluR5, mGlur, Group, I, Receptors, Glutamate, Metabotropic, antipsychotic, absence, epilepsy, PAM, (Metabotropic), 4323, Tocris Bioscience
2 Citations for VU 0360172 hydrochloride
Citations are publications that use Tocris products. Selected citations for VU 0360172 hydrochloride include:
Hanak et al (2019) Positive modulation of mGluR5 attenuates seizures and reduces TNF-α+ macrophages and microglia in the brain in a murine model of virus-induced temporal lobe epilepsy. Exp.Neurol. 311 194 PMID: 30316834
Bogdan A et al (2021) Enhanced Akt/GSK-3β/CREB signaling mediates the anti-inflammatory actions of mGluR5 positive allosteric modulators in microglia and following traumatic brain injury in male mice. J Neurochem 156 225-248 PMID: 31926033
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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
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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