1. GPCR/G Protein Neuronal Signaling
  2. mAChR
  3. Lu AE51090

Lu AE51090 是一种选择性的毒蕈碱 M1 受体激动剂,具有血脑屏障渗透性。Lu AE51090 激活人 M1 receptor,其 EC50 值为 61 nM,同时对 M2-M5 受体无显著激动作用。Lu AE51090 在小鼠中表现出促认知效应。Lu AE51090 可用于阿尔茨海默病 (AD) 和精神分裂症相关认知障碍 (CIAS) 研究。

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Lu AE51090

Lu AE51090 Chemical Structure

CAS No. : 1186229-95-7

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查看 mAChR 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Lu AE51090 is selective muscarinic M1 receptor agonist with blood-brain barrier penetration. Lu AE51090 activates human M1 receptor with EC50 of 61 nM, while showing no significant agonism at M2-M5 receptors. Lu AE51090 exerts procognitive effects in mice. Lu AE51090 can be used for the study of Alzheimer’s disease (AD) and cognitive impairment associated with schizophrenia (CIAS)[1].

IC50 & Target[1]

mAChR1

61 nM (EC50)

mAChR2

2200 nM (Ki)

mAChR3

7000 nM (Ki)

mAChR4

6900 nM (Ki)

mAChR5

8900 nM (Ki)

体外研究
(In Vitro)

Lu AE51090 (up to 10 μM) 在使用表达相应受体的 CHO-K1/BHK-21 细胞进行的 Ca2+ 动员实验中,对人 M1 受体表现出激动活性 (EC50 = 61 nM, Emax = 83%)[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Lu AE51090 (0.31-20 mg/kg,皮下注射,一次,实验前 30 分钟) 在雄性 C57Bl/6J 小鼠中以剂量依赖方式发挥促认知效应[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male C57Bl/6J mice (22-24 g)[1]
Dosage: 0.31, 1.3, 10, 20 mg/kg
Administration: s.c., once, 30 min pre-experiment
Result: Achieved dose-dependent reversal of delay-induced memory decay.
分子量

407.51

Formula

C24H29N3O3

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
Lu AE51090
目录号:
HY-118363
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