Aclidinium bromide
Aclidinium bromide
CAS: 320345-99-1
Molecular Formula: C13H10BrN
Aclidinium bromide - Names and Identifiers
| Name | Aclidinium bromide |
| Synonyms | LAS 34273 LAS-W 330 Unii-uqw7uf9N91 acridinium bromide Adiguanium bromide ACLIDINIUM BROMIDE Aclidinium bromide ACLIDINIUM BROMIDE INTERMEDIATES (3R)-(2-Hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane bromide 1-Azoniabicyclo(2.2.2)octane, 3-((hydroxydi-2-thienylacetyl)oxy)-1-(3-phenoxypropyl)-, bromide, (3R)- |
| CAS | 320345-99-1 |
| EINECS | 825-171-6 |
| InChI | InChI=1/C13H9N.BrH/c1-3-7-12-10(5-1)9-11-6-2-4-8-13(11)14-12;/h1-9H;1H |
Aclidinium bromide - Physico-chemical Properties
| Molecular Formula | C13H10BrN |
| Molar Mass | 564.56 |
| Melting Point | 230 °C(Solv: acetonitrile (75-05-8)) |
| Solubility | DMSO (Slightly, Heated), Methanol (Slightly) |
| Appearance | Solid |
| Color | White to Pale Orange |
| Storage Condition | under inert gas (nitrogen or Argon) at 2–8 °C |
| In vitro study | [Aclidinium is hydrolyzed in plasma samples of all species. At 37°C, in plasma of rat, guinea pig, dog and human, the apparent half-life is 11.7 minutes, 38.3 minutes, 1.8 minutes and 2.4 minutes. In human bronchial fibroblasts, Aclidinium (0.1 μm) inhibited acetylcholine and tgf-β1-induced up-regulation of type Ⅰ collagen and inhibited α-SMA mRNA and protein expression. In human bronchial fibroblasts, Aclidinium (0.1 μm) inhibited the tgf-β1-induced upregulation of ChAT expression. In human bronchial fibroblasts, Aclidinium (0.1 μm) inhibited the acetylcholine-and tgf-β1-induced increase in ERK1/2 phosphorylation and RhoA-GTP formation. In human lung fibroblasts, Aclidinium pretreatment prevented up-regulation of M1 and M3, but did not affect acetylcholine or tgf-β1-induced down-regulation of M2. In human lung fibroblasts, Aclidinium (0.1 μm) dose-dependently inhibited cell proliferation induced by TGF-β1 and acetylcholine. |
| In vivo study | In an acetylcholine-induced bronchoconstriction model in anesthetized guinea pigs, Aclidinium showed an initiating effect with an IC50 (95% CI) of 140 μg/ml and a t max of 30 min. In conscious beagle dogs, Aclidinium (500 μg/kg) induced a maximum 55% increase in heart rate 1 h after administration. In anesthetized guinea pigs, Aclidinium (1 mg/ml) produced an effective and durable tracheal protection (72%-88.4%) over the 120 min study period. |
Aclidinium bromide - Reference Information
| overview | when aclidinium bromide combined with long-acting selective adrenergic β2 receptor agonist formoterol (aclidinium bromide 400ug with formoterol 12ug, powder inhalation, BID) is applied to treat COPD, better curative effect will be obtained, and the lung function of patients will be better improved, the acute exacerbation rate is further reduced and can more effectively improve the quality of life of COPD patients. However, it was also pointed out that although aclidinium bromide combined with formoterol is more effective in the treatment of COPD, its safety must be further verified by further clinical studies |
| biological activity | Aclidinium Bromide (LAS 34273, LAS-W 330) binds to human muscarinic receptors AChR M1, M2, M3, M4 and M5 with Ki values of 0.1 nM, 0.14 nM, 0.14 nM, 0.21 nM and 0.16 nM respectively. |
| Target | Value |
| M1 mAChR | 0.1 nM(Ki) |
| M2 mAChR | 0.14 nM(Ki) |
| M3 mAChR | 0.14 nM(Ki) |
| M5 mAChR | 0.16 nM(Ki) |
| M4 mAChR | 0.21 nM(Ki) |
Last Update：2024-04-09 02:00:08
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