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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. | ||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+90% Corn Oil: 2 mg/mL (6.55 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
Ethanol/DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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