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VU0357121, a positive allosteric modulator of mGlu5 (EC50: 33 nM), is inactive or very weakly antagonizing at other mGlu receptor subtypes.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 2 mg | $35 | In Stock | In Stock | |
| 5 mg | $54 | In Stock | In Stock | |
| 10 mg | $87 | In Stock | In Stock | |
| 25 mg | $185 | In Stock | In Stock | |
| 50 mg | $296 | In Stock | In Stock | |
| 100 mg | $463 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $54 | In Stock | In Stock |
| Description | VU0357121, a positive allosteric modulator of mGlu5 (EC50: 33 nM), is inactive or very weakly antagonizing at other mGlu receptor subtypes. |
| Targets&IC50 | mGluR5:30 nM(EC50) |
| In vitro | VU0357121 do not bind at the MPEP allosteric site of mGlu5, thus do not possess mGlu5 NAM activity. The A809V/rmGlu5 mutation inhibited the ability of VU0357121 to shift the glutamate concentration?response curve, whereas the response to VU0357121 is not altered by the F585I/rmGlu5 mutation. [1] VU0357121 show weaker cooperativity in the Ca2+ mobilization assay in the low-expressing HEK293A-mGlu5 cell line. [2] |
| Molecular Weight | 305.32 |
| Formula | C17H17F2NO2 |
| Cas No. | 433967-28-3 |
| Smiles | CCCCOC1=CC=C(C=C1)C(=O)NC1=CC=C(F)C=C1F |
| Relative Density. | 1.220 g/cm3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | Ethanol: 30.5 mg/mL (99.9 mM), Sonication is recommended. DMSO: 30.5 mg/mL (99.9 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
Ethanol/DMSO
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