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Aceclidine

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货号 T19870Cas号 827-61-2

别名 Quinuclidin-3-yl acetate, NSC-657843, NSC657843, NSC 657843, Glaucostat, 3-quinuclidinyl acetate, 3-Acetoxyquinuclidine, 1-azabicyclo[2.2.2]octan-3-yl acetate

Aceclidine (1-azabicyclo[2.2.2]octan-3-yl acetate) 是M3 mAChR 的调节剂,可用于有关通过降低眼内压治疗青光眼的研究。

Aceclidine
其他形式的 “Aceclidine”:

Aceclidine

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Rating icon 很棒
货号 T19870 别名 Quinuclidin-3-yl acetate, NSC-657843, NSC657843, NSC 657843, Glaucostat, 3-quinuclidinyl acetate, 3-Acetoxyquinuclidine, 1-azabicyclo[2.2.2]octan-3-yl acetateCas号 827-61-2

Aceclidine (1-azabicyclo[2.2.2]octan-3-yl acetate) 是M3 mAChR 的调节剂,可用于有关通过降低眼内压治疗青光眼的研究。

规格价格库存数量
200 mg
¥ 99
现货
1 mL x 10 mM (in DMSO)
¥ 113
现货
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产品介绍


Aceclidine AI Summary
Aceclidine exhibits a range of bioactivities primarily targeting muscarinic acetylcholine receptors and phosphoinositol metabolism. It demonstrates strong binding affinity to the muscarinic acetylcholine receptor M1, with an IC50 of 120 nM using [3H]oxotremorine-M radioligand in rat hippocampus membranes, and a lower binding affinity (IC50 of 2427 nM) with [3H]pirenzepine radioligand. At 100 µM, it stimulates phosphoinositol (PI) hydrolysis by 60.5% in A9 L cells transfected with M1 receptors, with an EC50 of 4466 nM. Additionally, it induces marked salivation or tremor in mice at a dose of 10 mg/kg (Score = 2.0). The compound also shows significant inhibition of [3H](R)-QNB binding to muscarinic receptors in rat brain membranes (IC50 of 510 nM) and an 80% agonist activity in PI metabolism assays in rat cerebral cortex slices. Against muscarinic receptor M3 in A9 L cells, it has an EC50 of 10000 nM and a maximum stimulation of 130%. Moreover, it demonstrates binding affinities with a Ki value of 16 nM for [3H]OXO-M in rat brain membranes and exhibits phosphoinositol stimulation responses of up to 300% in rat hippocampal slices with an EC50 of 21000 nM. Additionally, Aceclidine shows antiviral activity against SARS-CoV-2, inhibiting cytotoxicity of VERO-6 cells at moderate concentrations, with varied IC50 values greater than 19952.62 nM. In other assays, it inhibits SARS-CoV-2 3CL-Pro protease by approximately 31.5% at 20 µM. The compound has inhibitory effects on the malarial parasite plastid (IC50 = 4775.5 nM) and RGS4 (IC50 = 42.3 nM), and displays growth inhibition in various human tumor cell lines, with notable potency against the A498 Renal cell line (GI50 = 3451.44 nM). Furthermore, it shows bioactivity related to toxicity in Musca domestica and affinity for muscarinic acetylcholine receptors in Drosophila melanogaster..
Note: Summary generated by AI. Data source: ChEMBL
生物活性
产品描述
Aceclidine (1-azabicyclo[2.2.2]octan-3-yl acetate) is a modulator of M3 mAChR and can be used in studies about treating glaucoma by reducing intraocular pressure.
别名Quinuclidin-3-yl acetate, NSC-657843, NSC657843, NSC 657843, Glaucostat, 3-quinuclidinyl acetate, 3-Acetoxyquinuclidine, 1-azabicyclo[2.2.2]octan-3-yl acetate
化学信息
分子量169.22
分子式C9H15NO2
CAS No.827-61-2
SmilesCC(=O)OC1CN2CCC1CC2
密度1.0873 g/cm3 (Estimated)
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
溶解度信息
H2O: 10 mg/mL (59.09 mM), Sonication is recommended.
DMSO: Soluble
溶液配制表
H2O
1mg5mg10mg50mg
1 mM5.9095 mL29.5473 mL59.0947 mL295.4733 mL
5 mM1.1819 mL5.9095 mL11.8189 mL59.0947 mL
10 mM0.5909 mL2.9547 mL5.9095 mL29.5473 mL
20 mM0.2955 mL1.4774 mL2.9547 mL14.7737 mL
50 mM0.1182 mL0.5909 mL1.1819 mL5.9095 mL

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

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 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% Saline / PBS / 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 100 μL DMSO ( 母液浓度为 20 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:100 μL DMSO 母液, 添加 400 μL PEG300 混匀澄清, 再加 50 μL Tween 80, 混匀澄清, 再加 450 μL Saline / PBS / ddH2O 混匀澄清
以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。
方案所需的各类助溶剂如: DMSOPEG300PEG400Tween 80SBE-β-CD玉米油等, 均可在TargetMol网站点击购买。
1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

剂量转换

对于不同动物的给药剂量换算,您也可以参考 更多

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