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Xanomeline (LY-246708) is a functionally selective M1/M4 activator used in the study of neurological disorders such as schizophrenia and has shown promising treatment in preclinical trials. Xanomeline is well absorbed orally, crosses the blood-brain barrier and undergoes extensive liver metabolism with at least six metabolites.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 2 mg | $30 | In Stock | In Stock | |
| 5 mg | $48 | In Stock | In Stock | |
| 10 mg | $81 | In Stock | In Stock | |
| 25 mg | $163 | In Stock | In Stock | |
| 50 mg | $263 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $53 | In Stock | In Stock |
| Description | Xanomeline (LY-246708) is a functionally selective M1/M4 activator used in the study of neurological disorders such as schizophrenia and has shown promising treatment in preclinical trials. Xanomeline is well absorbed orally, crosses the blood-brain barrier and undergoes extensive liver metabolism with at least six metabolites. |
| In vitro | In binding studies pre-incubating cells for one hour with 1 μM xanomeline, but not carbachol, reduced N-[3H]methylscopolamine saturation binding affinity but not maximal receptor density in cells [1]. |
| In vivo | Animal studies have shown the role of M4 and M1 receptors in modulating psychotic and behavioral disturbances and correction of negative and/or cognitive symptoms, respectively. The time to reach maximum plasma concentration (Tmax) for xanomeline is 2.5 hours, and maximum plasma concentration following xanomeline 150mg is 13.8ng/mL. Xanomeline is widely distributed, including to the CNS in animal studies, and the majority of the drug is excreted via the kidneys within 24 hours of administration[2]. |
| Synonyms | LY-246708 |
| Molecular Weight | 281.42 |
| Formula | C14H23N3OS |
| Cas No. | 131986-45-3 |
| Smiles | CCCCCCOc1nsnc1C1=CCCN(C)C1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||
| Solubility Information | DMSO: 4.5 mg/mL (15.99 mM), Sonication is recommended. | ||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (3.55 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 | |||||||||||||||||||||
DMSO
| |||||||||||||||||||||
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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