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Aclidinium bromide

Aclidinium bromide

产品编号 T2555   CAS 320345-99-1
别名: LAS 34273, LAS-W 330, 阿地溴铵

Aclidinium bromide (LAS-W 330) 是长效可吸入型的毒蕈碱拮抗剂,有用于慢性阻塞性肺病 (COPD) 的研究潜力。

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Aclidinium bromide Chemical Structure
Aclidinium bromide, CAS 320345-99-1
规格 价格/CNY 货期 数量
2 mg ¥ 297 现货
5 mg ¥ 496 现货
10 mg ¥ 788 现货
25 mg ¥ 1,430 现货
50 mg ¥ 2,450 现货
100 mg ¥ 3,680 现货
500 mg ¥ 8,270 现货
1 mL * 10 mM (in DMSO) ¥ 618 现货
产品目录号及名称: Aclidinium bromide (T2555)
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Aclidinium bromide (LAS-W 330) is a synthetic anticholinergic agent that is used as an inhalant for treatment of acute bronchospasm due to chronic bronchitis or emphysema. Aclidinium has not been implicated in causing liver enzyme elevations or clinically apparent acute liver injury.
靶点活性 M2 mAChR:0.14 nM(Ki), M4 mAChR:0.21 nM(Ki), M3 mAChR:0.14 nM(Ki), M1 mAChR:0.1 nM(Ki), M5 mAChR:0.16 nM(Ki)
体外活性 500 μg/kg Aclidinium给药1小时后诱导有意识的比格犬心率最大增加55%.1 mg/mL Aclidinium在超过120分钟的研究期间,产生对麻醉的豚鼠有效持久的气管保护作用(72%–88.4%).在麻醉的豚鼠的乙酰胆碱诱导的支气管收缩模型中,[3H] AcliAclidinium显示作用开始,IC50(95%CI)为140 μg/ mL,tmax为30分钟.
体内活性 Aclidinium在所研究的所有物种的血浆样品中均被水解,37℃下,在大鼠,豚鼠,狗和人的血浆中,表观半衰期分别为11.7分钟,38.3分钟,1.8分钟和2.4分钟。0.1 μM Aclidinium抑制人支气管成纤维细胞中乙酰胆碱和TGF-β1诱导的Ⅰ型胶原上调,并抑制α-SMA mRNA和蛋白质表达。0.1 μM Aclidinium抑制碳酰胆碱和TGF-β1诱导的人支气管成纤维细胞中ERK1/2磷酸化和RhoA-GTP形成的增加。0.1 μM Aclidinium抑制TGF-β1诱导的人支气管成纤维细胞中ChAT表达的上调。0.1 μM Aclidinium在剂量依赖性地抑制人肺成纤维细胞的TGF-β1和卡巴胆碱诱导的细胞增殖。< 100 nM Aclidinium剂量依赖性抑制豚鼠离体豚鼠气管中卡巴胆碱诱导的收缩。Aclidinium预处理可阻止人肺成纤维细胞中M1和M3的上调,但不能抑制由碳酰胆碱或TGF-β1诱导的M2的下调。
激酶实验 Affinity assay: The affinity of Aclidinium for the different human muscarinic receptor subtypes at equilibrium is determined by measuring their ability to displace the binding of [3H]NMS to cell membrane preparations expressing one of the human muscarinic receptor subtypes. Protein concentrations are 8.1 μg/well, 10.0 μg/well, 4.9 μg/well, 4.5 μg/well, and 5.0 μg/well for M1, M2, M3, M4, and M5 receptor membrane preparations, respectively. The assays are conducted at [3H]NMS concentrations approximately equal to the radioligand equilibrium dissociation constant (Kd) for the different muscarinic receptors subtypes. The [3H]NMS concentration is 0.3 nM for the M1 and M4 assays and 1 nM for the M2, M3, and M5 assays. A range of antagonist concentrations (10?14 to 10?5 M) are tested in duplicate to generate competition curves. Nonspecific binding is determined in the presence of atropine (1 μM). Assay reagents are dissolved in assay binding buffer (phosphate-buffered saline with calcium and magnesium) to a total volume of 200 μL. After a 2 hours or 6 hours incubation period (M1–M4 and M5, respectively) at room temperature in 96-well microtiter plates to ensure that equilibrium is achieved for Aclidinium, 150 μL aliquots of the reaction are transferred to GF/C filter plates pretreated for 1 hour with wash buffer (50 mM Tris, 100 mM NaCl, pH 7.4) containing 0.05% polyethylenimine. Bound and free [3H]NMS are then separated by rapid vacuum filtration followed by four washes with ice-cold wash buffer. Filters are then dried for 30 min before addition of 30 μL of OptiPhase Supermix, and radioactivity is quantified using a MicroBeta Trilux microplate scintillation counter.
细胞实验 Human bronchial fibroblast proliferation is measured as previously outlined by colorimetric immunoassay based on BrdU incorporation during DNA synthesis using a cell proliferation enzyme-linked immunosorbent assay BrdU kit according to the manufacturer's protocol. Cells are seeded at a density of 3x103 cells/well on 96-well plates and incubated for 24 hours. Cells are then exposed to different experimental conditions. The 490 nm absorbance is quantified using a microplate spectrophotometer. Proliferation data refers to the absorbance values of BrdU-labeled cellular DNA content per well. Stimulation is expressed as x-fold proliferation over basal growth of the untreated control set as unity.(Only for Reference)
别名 LAS 34273, LAS-W 330, 阿地溴铵
分子量 564.55
分子式 C26H30NO4S2·Br
CAS No. 320345-99-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 104 mg/mL (184.2 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7713 mL 8.8566 mL 17.7132 mL 44.2831 mL
5 mM 0.3543 mL 1.7713 mL 3.5426 mL 8.8566 mL
10 mM 0.1771 mL 0.8857 mL 1.7713 mL 4.4283 mL
20 mM 0.0886 mL 0.4428 mL 0.8857 mL 2.2142 mL
50 mM 0.0354 mL 0.1771 mL 0.3543 mL 0.8857 mL
100 mM 0.0177 mL 0.0886 mL 0.1771 mL 0.4428 mL

计算器

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稀释计算器
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分子量计算器
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参考文献

1. Gavaldà A, et al. J Pharmacol Exp Ther, 2009, 331(2), 740-751. 2. Sentellas S, et al. Eur J Pharm Sci, 2010, 39(5), 283-290. 3. Milara J, et al. Thorax, 2012, 67(3), 229-237.
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相关化合物库

该产品包含在如下化合物库中:
神经退行性疾病化合物库 已知活性化合物库 FDA 上市药物库 抑制剂库 药物功能重定位化合物库 NO PAINS 化合物库 ReFRAME 相关化合物库 抗阿尔茨海默症化合物库 经典已知活性库 神经递质受体化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

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。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步: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
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% ddH2O
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技术支持

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。

Keywords

Aclidinium bromide 320345-99-1 Neuroscience AChR inhibit LAS-34273 Muscarinic acetylcholine receptor Aclidinium Bromide LAS 34273 LAS-W 330 mAChR 阿地溴铵 Inhibitor LAS-W330 LAS34273 LAS-W-330 Aclidinium inhibitor

 

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