| Description | LY2389575 hydrochloride is an mGlu3 negative allosteric modulator (NAM) that is selective and non-competitive, with an IC50 value of 190 nM. LY2389575 hydrochloride induces an increase in the level of Mrc1, which amplifies the toxicity of β-amyloid (Aβ), and can be used to study Alzheimer's disease. It can be used to study Alzheimer's disease. |
| In vitro | LY2389575 hydrochloride (5 μM; 1 h) 促进小胶质细胞中Mrc1水平的增加。[2] |
| Target activity | mGluR3:190 nM |
| molecular weight | 438.58 |
| Molecular formula | C15H16BrCl3N4 |
| CAS | 885104-09-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 90.0 mg/mL (205.2 mM), Sonication and heating to 60℃ are recommended. Methanol: 7.5 mg/mL (17.1 mM), Sonication and heating to 60℃ are recommended. |
| References | 1. Caraci F, et al. 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 mGlu2 and mGlu3 receptors is neuroprotective. Mol Pharmacol. 2011;79(3):618-626. 2. Zinni M, et al. mGlu3 receptor regulates microglial cell reactivity in neonatal rats. J Neuroinflammation. 2021;18(1):13. 3. Srivastava A, et al. Metabotropic Glutamate Receptors in Alzheimer's Disease Synaptic Dysfunction: Therapeutic Opportunities and Hope for the Future. J Alzheimers Dis. 2020;78(4):1345-1361. 4. Sheffler DJ, et al. Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) derived from a closely related mGlu5 PAM. Bioorg Med Chem Lett. 2012;22(12):3921-3925. |