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VU0361737

🥰Excellent
Catalog No. T6726Cas No. 1161205-04-4
Alias VU 0361737, ML-128

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.

VU0361737

VU0361737

🥰Excellent
Purity: 99.86%
Catalog No. T6726Alias VU 0361737, ML-128Cas No. 1161205-04-4
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 SizePriceAvailabilityQuantity
10 mg$30In Stock
25 mg$56In Stock
50 mg$94In Stock
100 mg$153In Stock
200 mg$225In Stock
1 mL x 10 mM (in DMSO)$29In Stock
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Purity:99.86%
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Product Introduction

Bioactivity
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.
AliasVU 0361737, ML-128
Chemical Properties
Molecular Weight262.69
FormulaC13H11ClN2O2
Cas No.1161205-04-4
SmilesCOc1cc(NC(=O)c2ccccn2)ccc1Cl
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM3.8068 mL19.0338 mL38.0677 mL190.3384 mL
5 mM0.7614 mL3.8068 mL7.6135 mL38.0677 mL
10 mM0.3807 mL1.9034 mL3.8068 mL19.0338 mL
20 mM0.1903 mL0.9517 mL1.9034 mL9.5169 mL
50 mM0.0761 mL0.3807 mL0.7614 mL3.8068 mL
100 mM0.0381 mL0.1903 mL0.3807 mL1.9034 mL

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