VU 0357121 (CAS 433967-28-3)
Application:
VU 0357121 is a novel allosteric modulator of mGluR-5 receptors
CAS Number:
433967-28-3
Molecular Weight:
305.32
Molecular Formula:
C17H17F2NO2
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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Description
Safety Information
SDS & Certificate of Analysis
VU0357121 is a novel allosteric modulator of mGlu5 receptors with EC50 of 33 nM. VU0357121 do not bind at the MPEP allosteric site of mGlu5, thus do not possess mGlu5 NAM activity.
VU 0357121 (CAS 433967-28-3) References
- Investigating metabotropic glutamate receptor 5 allosteric modulator cooperativity, affinity, and agonism: enriching structure-function studies and structure-activity relationships. | Gregory, KJ., et al. 2012. Mol Pharmacol. 82: 860-75. PMID: 22863693
- Optimization of an ether series of mGlu5 positive allosteric modulators: molecular determinants of MPEP-site interaction crossover. | Manka, JT., et al. 2012. Bioorg Med Chem Lett. 22: 6481-5. PMID: 22981332
- Discovery and SAR of a novel series of non-MPEP site mGlu₅ PAMs based on an aryl glycine sulfonamide scaffold. | Rodriguez, AL., et al. 2012. Bioorg Med Chem Lett. 22: 7388-92. PMID: 23142615
- A novel metabotropic glutamate receptor 5 positive allosteric modulator acts at a unique site and confers stimulus bias to mGlu5 signaling. | Noetzel, MJ., et al. 2013. Mol Pharmacol. 83: 835-47. PMID: 23348500
- Progress toward advanced understanding of metabotropic glutamate receptors: structure, signaling and therapeutic indications. | Yin, S. and Niswender, CM. 2014. Cell Signal. 26: 2284-97. PMID: 24793301
- Therapeutic molecules and endogenous ligands regulate the interaction between brain cellular prion protein (PrPC) and metabotropic glutamate receptor 5 (mGluR5). | Haas, LT., et al. 2014. J Biol Chem. 289: 28460-77. PMID: 25148681
- Cocaine Decreases Metabotropic Glutamate Receptor mGluR1 Currents in Dopamine Neurons by Activating mGluR5. | Kramer, PF. and Williams, JT. 2015. Neuropsychopharmacology. 40: 2418-24. PMID: 25829143
- Identification of Novel Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5 Acting at Site Distinct from 2-Methyl-6-(phenylethynyl)-pyridine Binding. | Butkiewicz, M., et al. 2019. ACS Chem Neurosci. 10: 3427-3436. PMID: 31132237
- Effect of small molecule signaling in PepFect14 transfection. | Gestin, M., et al. 2020. PLoS One. 15: e0228189. PMID: 31999754
Activator of:
mGluR-5.Substrate of:
mGluR.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
VU 0357121, 10 mg | sc-364645 | 10 mg | $145.00 | |||
VU 0357121, 50 mg | sc-364645A | 50 mg | $615.00 |