Biological Activity
Selective negative allosteric modulator of mGlu3 (IC50 = 190 nM). Exhibits > 65-fold selectivity for mGlu3 over other mGlu receptors. Abolishes the neuroprotective action of LY 379268 against amyloid β toxicity in mixed cortical neuronal and astrocyte cell cultures.
Technical Data
| M. Wt | 438.58 |
| Formula | C15H15BrCl2N4.HCl |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 885104-09-6 |
| PubChem ID | 11503054 |
| InChI Key | IRIBLLOEUZMCQY-ZOWNYOTGSA-N |
| Smiles | ClC1=CC(Cl)=CC=C1CN[C@@H]2CN(C3=NC=C(Br)C=N3)CC2.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 | 8.77 | 20 |
Preparing Stock Solutions
The following data is based on the product molecular weight 438.58. 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 | 2.28 mL | 11.4 mL | 22.8 mL |
| 5 mM | 0.46 mL | 2.28 mL | 4.56 mL |
| 10 mM | 0.23 mL | 1.14 mL | 2.28 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.46 mL |
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References
References are publications that support the products' biological activity.
Caraci et al (2011) Targeting group II metabotropic glutamate (mGlu) receptors for the treatment of psychosis associated with Alzheimer's disease: selective activation of mGlu2 receptors amplifies beta-amyloid toxicity in cultured neurons, whereas dual activation of mGl Mol.Pharmacol. 79 618 PMID: 21159998
Keywords: LY 2389575 hydrochloride, supplier, LY2389575, hydrochloride, selective, negative, allosteric, modulators, NAM, group, II, 2, glutamate, receptors, mGlu3, Glutamate, (Metabotropic), Group, II, Receptors, Glutamate, (Metabotropic), Group, II, Receptors, Tocris Bioscience
