Name | VU 0357121 |
Synonyms | SKL855 CS-1971 VU 0357121 4-Butoxy-N-(2,4-difluorophenyl)benzamide BenzaMide, 4-butoxy-N-(2,4-difluorophenyl)- |
CAS | 433967-28-3 |
Molecular Formula | C17H17F2NO2 |
Molar Mass | 305.32 |
Density | 1.220 |
Boling Point | 338.7±42.0 °C(Predicted) |
Solubility | DMSO: ≥18mg/mL |
Appearance | powder |
pKa | 11.74±0.70(Predicted) |
Storage Condition | 2-8°C |
MDL | MFCD03243692 |
Use | VU0357121 |
In vitro study | VU0357121 has no PAM activity to other mGluR subtypes, nor does it bind to the MPEP conformation site of mGlu 5, so it does not have mGlu 5 NAM activity. The A809V/r mGlu5 mutation inhibited the activity of VU0357121 and altered the glutamate concentration-response curve without affecting the activity associated with the F585I/r mGlu5 mutation. Ca2 mobilization assay showed that the activity of VU0357121 was low in cell lines with low expression of HEK293A-mGlu5. |
Hazard Symbols | N - Dangerous for the environment |
Risk Codes | 50/53 - Very toxic to aquatic organisms, may cause long-term adverse effects in the aquatic environment. |
Safety Description | S60 - This material and its container must be disposed of as hazardous waste. S61 - Avoid release to the environment. Refer to special instructions / safety data sheets. |
UN IDs | UN 3077 9 / PGIII |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.275 ml | 16.376 ml | 32.753 ml |
5 mM | 0.655 ml | 3.275 ml | 6.551 ml |
10 mM | 0.328 ml | 1.638 ml | 3.275 ml |
5 mM | 0.066 ml | 0.328 ml | 0.655 ml |
biological activity | VU 0357121 is a novel positive allosteric modulator (PAM) of mGlu5 with an EC50 of 33 nM, the activity of other mGlu receptor subtypes is inhibited or rendered very low. |