Aclidinium bromide

SKU: orb1305321

Description

Aclidinium bromide is a synthetic anticholinergic agent used in research to study bronchodilation for conditions like COPD. It is applied in both in vitro receptor binding assays and in vivo models of bronchospasm to investigate muscarinic antagonism and airway physiology.

Research Area

Neuroscience

Images & Validation

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Key Properties

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CAS Number	320345-99-1
MW	564.55
Purity	99.53%
Formula	C₂₆H₃₀NO₄S₂·Br
SMILES	[Br-].OC(C(=O)O[C@H]1C[N+]2(CCCOc3ccccc3)CCC1CC2)(c1cccs1)c1cccs1
Target	AChR
Solubility	DMSO:104 mg/mL (184.22 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (7.09 mM)

Bioactivity

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Target IC50	M1 mAChR:0.1 nM(Ki)\|M5 mAChR:0.16 nM(Ki)\|M3 mAChR:0.14 nM(Ki)\|M4 mAChR:0.21 nM(Ki)\|M2 mAChR:0.14 nM(Ki)
In Vivo	Administering 500 μg/kg of Aclidinium resulted in a maximum increase of 55% in the heart rate of conscious Beagles one hour after dosage. A concentration of 1 mg/mL of Aclidinium showed effective and sustained tracheal protection (72%–88.4%) in anesthetized guinea pigs over a study period exceeding 120 minutes. In a model of acetylcholine-induced bronchoconstriction in anesthetized guinea pigs, [3H]Aclidinium demonstrated onset of action with an IC50 (95% CI) of 140 μg/mL and a tmax of 30 minutes. Read more...
In Vitro	Aclidinium is hydrolyzed in plasma samples across all studied species at 37°C, with apparent half-lives of 11.7 minutes in rats, 38.3 minutes in guinea pigs, 1.8 minutes in dogs, and 2.4 minutes in humans. At a concentration of 0.1 μM, Aclidinium inhibits the upregulation of Type I collagen induced by acetylcholine and TGF-β1 in human bronchial fibroblasts, as well as suppressing the expression of α-SMA mRNA and protein. Additionally, 0.1 μM Aclidinium inhibits the increase in ERK1/2 phosphorylation and RhoA-GTP formation triggered by carbachol and TGF-β1 in human bronchial fibroblasts. It also represses the upregulation of ChAT expression induced by TGF-β1. A dose-dependent inhibition of TGF-β1 and carbachol-induced proliferation in human lung fibroblasts is observed with 0.1 μM Aclidinium. Concentrations below 100 nM dose-dependently inhibit carbachol-induced contraction in isolated guinea pig trachea. Pre-treatment with Aclidinium prevents the upregulation of M1 and M3 receptors in human lung fibroblasts but does not inhibit the downregulation of M2 induced by carbachol or TGF-β1. Read more...
Cell Research	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) Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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Inhibitor, LAS34273, LAS-34273, LAS 34273, LAS-W 330, LAS-W330, LAS-W-330, M2 mAChR, M3 mAChR, M1 mAChR, mAChR, M4 mAChR, M5 mAChR, Muscarinic acetylcholine receptor, inhibit, Aclidinium, Aclidinium Bromide, Aclidinium bromide

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Compound Identifiers

PubChem CID

11519741 ↗

Key Properties

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No computed properties available.

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