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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 | Availability | Quantity |
---|---|---|---|
5 mg | $50 | In Stock | |
10 mg | $96 | In Stock | |
25 mg | $168 | In Stock | |
50 mg | $298 | In Stock | |
100 mg | $489 | In Stock | |
1 mL x 10 mM (in DMSO) | $60 | 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]. |
Alias | LY-246708 |
Molecular Weight | 281.42 |
Formula | C14H23N3OS |
Cas No. | 131986-45-3 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
Solubility Information | DMSO: 4.5 mg/mL (15.99 mM), Sonication is recommended. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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