Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Xanomeline (LY-246708) 是一种功能性选择性 M1/M4激活剂,用于精神分裂等神经疾病的研究,在临床前试验中显示出良好的治疗前景。Xanomeline 口服吸收良好,通过血脑屏障,并与至少六种代谢物进行广泛的肝脏代谢。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 217 | 现货 | ||
5 mg | ¥ 479 | 现货 | ||
10 mg | ¥ 828 | 现货 | ||
25 mg | ¥ 1,660 | 现货 | ||
50 mg | ¥ 2,650 | 现货 | ||
100 mg | ¥ 3,950 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 538 | 现货 |
产品描述 | 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. |
体外活性 |
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]. |
体内活性 | 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]. |
别名 | LY-246708 |
分子量 | 281.42 |
分子式 | C14H23N3OS |
CAS No. | 131986-45-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 45.0 mg/mL (159.9 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.5534 mL | 17.767 mL | 35.5341 mL | 88.8352 mL |
5 mM | 0.7107 mL | 3.5534 mL | 7.1068 mL | 17.767 mL | |
10 mM | 0.3553 mL | 1.7767 mL | 3.5534 mL | 8.8835 mL | |
20 mM | 0.1777 mL | 0.8884 mL | 1.7767 mL | 4.4418 mL | |
50 mM | 0.0711 mL | 0.3553 mL | 0.7107 mL | 1.7767 mL | |
100 mM | 0.0355 mL | 0.1777 mL | 0.3553 mL | 0.8884 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Xanomeline 131986-45-3 Neuroscience AChR LY246708 LY 246708 LY-246708 Inhibitor inhibitor inhibit