Biological Activity
Potent and selective negative allosteric modulator of mGlu1 (IC50 = 99 nM). Exhibits >100-fold selectivity for mGlu1 over mGlu2-8 and 68 other GPCRs, ion channels, kinases and transporters. Brain penetrant.
Technical Data
| M. Wt | 400.94 |
| Formula | C22H28N4O.HCl |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1443748-47-7 |
| PubChem ID | 71680759 |
| InChI Key | YENVAZRENOYZGQ-GUIQYPADSA-N |
| Smiles | O=C(N4CCN(C5=C(C#N)N=CC=C5)C[C@H]4C)C12CC(C3)CC(CC3C2)C1.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 40.09 | 100 | |
| ethanol | 20.05 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 400.94. Batch specific molecular weights may vary from batch to batch due to solvent 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 | 2.49 mL | 12.47 mL | 24.94 mL |
| 5 mM | 0.5 mL | 2.49 mL | 4.99 mL |
| 10 mM | 0.25 mL | 1.25 mL | 2.49 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.5 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Lovell et al (2013) N-Acyl-N'-arylpiperazines as negative allosteric modulators of mGlu1: Identification of VU0469650, a potent and selective tool compound with CNS exposure in rats. Bioorg.Med.Chem.Lett. 23 3713 PMID: 23727046
Keywords: VU 0469650 hydrochloride, supplier, VU0469650, hydrochloride, modulators, metabotropic, glutamate, receptor, mGlu1, mGluR1, allosteric, negative, potent, selective, NAMs, Glutamate, (Metabotropic), Group, I, Receptors, Glutamate, (Metabotropic), Group, I, Receptors, Tocris Bioscience
