Molecular Formula | C13H11ClN2O2 |
Molar Mass | 262.69 |
Solubility | DMSO: soluble15mg/mL (clear solution) |
Appearance | film |
Color | white |
Storage Condition | Inert atmosphere,2-8°C |
MDL | MFCD16618402 |
Use | VU0361737 |
In vitro study | VU0361737 is inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors and displays weak activity at mGlu5 and mGlu8 receptors. |
In vivo study | 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). |
Hazard Symbols | Xn - Harmful |
Risk Codes | R22 - Harmful if swallowed R36 - Irritating to the eyes |
Safety Description | 26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.807 ml | 19.034 ml | 38.068 ml |
5 mM | 0.761 ml | 3.807 ml | 7.614 ml |
10 mM | 0.381 ml | 1.903 ml | 3.807 ml |
5 mM | 0.076 ml | 0.381 ml | 0.761 ml |
biological activity | VU 0361737 is a selective (PAM)mGlu4 receptor positive allosteric modulator (PAM), which acts on human and rat receptors. EC50 is 240 nM and 110 nM respectively. It has weak activity on mGlu5 and mGlu8 receptors and inhibits mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptor activity, can penetrate into the CNS. |
in vitro study | VU0361737 is inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors and displays weak activity at mGlu5 and mGlu8 receptors. |
in vivo study | 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). |
target | human mGlu 4 240 nM (EC 50 ) Rat mGlu 4 110 nM (EC 50 ) |