| Name | VU0361737 |
| Description | VU0361737 (ML-128) is a specific positive allosteric modulator (PAM) of the mGlu4 receptor with an EC50 of 240 nM for human receptors and 110 nM for rat receptors. It exhibits weak activity at mGlu5 and mGlu8 receptors and is inactive at mGlu1, mGlu2, mGlu3, mGlu6, and mGlu7 receptors. The compound can penetrate the CNS. |
| Kinase Assay | Enzyme Assays: The enzymatic activities of NAMPT and NMNAT are measured using in vitro kits and using the Two-Step Method per manufacturer's instructions. Compounds, NAMPT and/or NMNAT enzymes, and their substrates are mixed and incubated at 30°C for 1 hour. Reagents for the indicator reaction (Wst-1) are then added, and absorbance is read at 450 nm every 5 min at 30°C on a Tecan In?nite M100 multimode plate reader. |
| In vitro | VU0361737 is inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors and displays weak activity at mGlu5 and mGlu8 receptors. [1] |
| In vivo | VU0361737 shows high in vivo CL in rat, a short half-life (T1/2 20 min), and demonstrates significant brain exposure (brain-to-plasma ratio of 4.1). [1] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 45 mg/mL (171.3 mM)
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| Keywords | Parkinson's | inhibit | neuroprotective | Metabotropic glutamate receptors | VU0361737 | VU-0361737 | Inhibitor | disease | ML 128 | mGluR | ML128 |
| Inhibitors Related | IDRA-21 | Topiramate | Decanoic Acid | Urethane | L-Cysteic acid monohydrate | Evans blue | L-Glutamine | Direct Blue 1 | L-Glutamic acid monosodium salt | Piracetam | O-Phospho-L-serine | Memantine hydrochloride |
| Related Compound Libraries | Bioactive Compound Library | Anti-Neurodegenerative Disease Compound Library | Neuronal Signaling Compound Library | Membrane Protein-targeted Compound Library | Glutamine Metabolism Compound Library | Anti-Parkinson's Disease Compound Library | Neurotransmitter Receptor Compound Library | Neuroprotective Compound Library | NO PAINS Compound Library | Bioactive Compounds Library Max |
United States
