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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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
10 mg | $30 | In Stock | |
25 mg | $56 | In Stock | |
50 mg | $94 | In Stock | |
100 mg | $153 | In Stock | |
200 mg | $225 | In Stock | |
1 mL x 10 mM (in DMSO) | $29 | In Stock |
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. |
Targets&IC50 | mGluR4 (rat):110 nM(EC50), mGluR4 (human):240 nM(EC50) |
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] |
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. |
Alias | VU 0361737, ML-128 |
Molecular Weight | 262.69 |
Formula | C13H11ClN2O2 |
Cas No. | 1161205-04-4 |
Smiles | COc1cc(NC(=O)c2ccccn2)ccc1Cl |
Relative Density. | no data available |
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) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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