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BMS-984923 is an orally available and blood-brain barrier permeable mGluR5 silencing allosteric modulator that inhibits β-amyloid oligomer-induced aberrant synaptic signaling, and can be used to study Alzheimer's disease.


| Description | BMS-984923 is an orally available and blood-brain barrier permeable mGluR5 silencing allosteric modulator that inhibits β-amyloid oligomer-induced aberrant synaptic signaling, and can be used to study Alzheimer's disease. |
| In vivo | BMS-984923 (7.5 mg/kg or 15 mg/kg, oral gavage, once) exhibited good oral bioavailability and BBB permeability in C57Bl6J male mice ( 7.5 mg/kg or 15 mg/kg, oral gavage, once); resulting in plasma concentrations exceeding 2 μM at 10 hours. Brain concentrations were almost as high as plasma concentrations when measured 3 hours after the 7.5 mg/kg oral dose [1]. |
| Synonyms | BMS984923, BMS 984923 |
| Molecular Weight | 374.82 |
| Formula | C22H15ClN2O2 |
| Cas No. | 1375752-78-5 |
| Smiles | ClC1=C([C@@H]2[C@H](NC(=O)O2)C=3C=C(C#CC4=CC=CC=C4)C=NC3)C=CC=C1 |
| Relative Density. | 1.38 g/cm3 (Predicted) |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 30 mg/mL (80.04 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.34 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 | |||||||||||||||||||||||||||||||
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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