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Muscarinic M4 modulator-1 is a positive allosteric modulator of the Muscarinic M4 receptor. It activates the muscarinic M4 receptor with allosteric efficacy (EC50) values of 14 nM in CHO-K1 cells and 3 nM in HEK293 cells. Muscarinic M4 modulator-1 exhibits antipsychotic-like activity and shows potential for research in psychiatric and/or neurological disorders.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
| Description | Muscarinic M4 modulator-1 is a positive allosteric modulator of the Muscarinic M4 receptor. It activates the muscarinic M4 receptor with allosteric efficacy (EC50) values of 14 nM in CHO-K1 cells and 3 nM in HEK293 cells. Muscarinic M4 modulator-1 exhibits antipsychotic-like activity and shows potential for research in psychiatric and/or neurological disorders. |
| In vitro | Muscarinic M4 modulator-1 (Example 4) exhibits allosteric efficacy on muscarinic M4 receptors with an EC50 of 14 nM in CHO-K1 cells and 3 nM in HEK293 cells (0.2-4 hours). |
| In vivo | Muscarinic M4 modulator-1 (Example 4), administered once via intraperitoneal injection at doses of 10 and 30 mg/kg in a rat model, showed receptor occupancy rates of 33.9% and 66.7%, respectively. |
| Molecular Weight | 412.44 |
| Formula | C21H22F2N6O |
| Cas No. | 3082186-91-9 |
| Smiles | O=C(N1CC=2C(=CC3=NC(=NN3C2C1)C)C)CC4CN(C=5C=CN=C(C5)C(F)F)C4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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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