阿地溴铵|T2555

Aclidinium bromide
320345-99-1

￥215 1mg 起订

￥496 5mg 起订

￥745 10mg 起订

上海更新日期：2024-09-14

TargetMol中国（陶术生物）

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联系人：邵小姐

电话：021-021-33632979拨打

手机：15002134094 拨打

邮箱：marketing@targetmol.com

产品详情:

中文名称：: 阿地溴铵

英文名称：: Aclidinium bromide

CAS号：: 320345-99-1

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.69%

产品类别：: 抑制剂

货号：: T2555

Product Introduction

Bioactivity

名称	Aclidinium bromide
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.
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)
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.
体外活性	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。
体内活性	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.
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
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)
关键字	inhibit \| LAS-34273 \| Muscarinic acetylcholine receptor \| Aclidinium Bromide \| mAChR \| Inhibitor \| Aclidinium bromide \| LAS-W330 \| LAS34273 \| LAS-W-330 \| Aclidinium
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阿地溴铵|||LAS-W 330|||LAS 34273|TargetMol

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