2. GPCR/G Protein Neuronal Signaling
  3. mAChR
  4. Milameline

Milameline  (Synonyms: CI-979; RU35926)

目录号: HY-135460
产品使用指南 技术支持

Milameline (CI-979; RU35926) 是一种非选择性、局部性、口服有效的毒蕈碱受体 (muscarinic receptor) 激动剂，可改善认知功能。Milameline 对不同亚型的人 muscarinic receptor 的亲和力相同，M1-、M2-、M3- 和 M4-muscarinic receptors 的 IC50 分别为1.3、1.1、1.5 和 1.9 µM。Milameline 对 [3H]CMD 位点的亲和力 (IC50 = 20 nM) 高于 [3H]QNB 位点 (IC50 = 3059 nM)。Milameline 可产生中枢和外周胆碱能作用，并逆转 Scopolamine (HY-N0296) 引起的认知缺陷。Milameline 可用于阿尔茨海默病的研究。

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Milameline

Milameline Chemical Structure

CAS No. : 139886-32-1

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Customer Review

Other Forms of Milameline:

Milameline 相关抗体

Top Publications Citing Use of Products

查看 mAChR 亚型特异性产品:

查看所有亚型
mAChR1 mAChR2 mAChR3 mAChR4 mAChR5

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Milameline (CI-979; RU35926) is a nonselective, partical and orally active muscarinic receptor agonist that improves cognition. Milameline has equal affinity for different subtypes of human muscarinic receptors with IC50 of 1.3 µM for M1-, 1.1 µM for M2-, 1.5 µM for M3-, and 1.9 µM for M4-muscarinic receptors. Milameline has a higher affinity for sites [3H]CMD (IC50 = 20 nM), than [3H]QNB, (IC50 = 3059 nM). Milameline produces both central and peripheral cholinergic effects and reverses the cognitive deficits induced by Scopolamine (HY-N0296). Milameline can be used for the study of Alzheimer’s Disease[1].

IC50 & Target[1]

mAChR1

1.3 μM (IC50)

mAChR2

1.1 μM (IC50)

mAChR3

1.5 μM (IC50)

mAChR4

1.9 μM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 EC50
0.021 μM
Compound: Milameline
Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
[PMID: 25765911]
体外研究
(In Vitro)

Milameline 增加了转染了人类 M1 或 M3 受体的 CHO 细胞中可溶性 APP (sAPP) 的分泌[1]。

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

Milameline 相关抗体:
体内研究
(In Vivo)

Milameline (0.2 mg/kg (大鼠), 口服, 或 0.01 mg/kg (猴), 肌注, 单次给药) 在大鼠中产生中枢效应 (体温过低) 并在猴中产生中枢胆碱能效应 (脑电图 (EEG) 中新皮层觉醒度增加)[1]。
Milameline (0.02- > 0.1 mg/kg, 口服) 在低剂量 (0.02-0.1 mg/kg) 下有效逆转 Scopolamine (HY-N0296) 诱导的大鼠工作记忆损伤，但在高剂量下 (> 0.1 mg/kg) 该效应减弱[1]。
Milameline 增加大鼠脑血流量，并且其在大脑中的分布与胆碱能系统富集的区域一致[1]。

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

154.21

Formula

C8H14N2O
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

Milameline 相关分类

  • 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.

Keywords:

Milameline139886-32-1CI-979 RU35926CI979CI 979RU35926RU 35926RU-35926mAChRMuscarinic acetylcholine receptorAlzheimer’s diseaseMuscarinic receptor agonistTetrahydropyridine aldoximePD-129409.Inhibitorinhibitorinhibit

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