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Description: Potent and selective negative allosteric modulator of mGlu2 receptors
Purity: ≥98% (HPLC)
Biological Activity for VU 6001966
VU 6001966 is a potent and selective mGlu2 negative allosteric modulator (IC50 = 78 nM). Exhibits > 350-fold selectivity for mGlu2 over mGlu3. Also exhibits selectivity over other mGluRs and a panel of GPCRs, ion channels and transporters. VU 6001966 induces antidepression like effects in mouse models of chronic stress. CNS penetrant.
Licensing Information
Sold under license from Vanderbilt University
Compound Libraries for VU 6001966
VU 6001966 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for VU 6001966
| M. Wt | 326.33 |
| Formula | C17H15FN4O2 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 2009052-76-8 |
| PubChem ID | 122539788 |
| InChI Key | SSSNPJKQBYVHBV-UHFFFAOYSA-N |
| Smiles | CN1C=CC(COC2=CN=C(C(N)=O)C=C2C3=CC=C(C=C3)F)=N1 |
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 6001966
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 32.63 | 100 | |
| ethanol | 1.63 | 5 |
Preparing Stock Solutions for VU 6001966
The following data is based on the product molecular weight 326.33. 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 6001966
References for VU 6001966
References are publications that support the biological activity of the product.
Bollinger et al (2017) Design and synthesis of mGlu2 NAMs with improved potency and CNS penetration based on a truncated picolinamide core. ACS Med.Chem.Lett. 8 919 PMID: 28947937
Joffe et al (2020) mGlu 2 and mGlu 3 negative allosteric modulators divergently enhance thalamocortical transmission and exert rapid antidepressant-like effects. Neuron 105 46 PMID: 31735403
If you know of a relevant reference for VU 6001966, please let us know.
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Keywords: VU 6001966, VU 6001966 supplier, VU6001966, metabotropic, glutamate, receptors, mGlu2, mGluR, mGlu2R, potent, selective, negative, allosteric, modulators, modulates, NAMs, CNS, penetrant, Glutamate, (Metabotropic), Group, II, Receptors, 6928, Tocris Bioscience
Citations for VU 6001966
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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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