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Purity: ≥98%
Aclidinium Bromide (formerly LAS34273, LAS-W 330; brand names Tudorza Genuair; Eklira Genuair; Bretaris Genuair) is a potent, long-acting and inhalable muscarinic antagonist used as a maintenance treatment for chronic obstructive pulmonary disease (COPD). It acts by potently inhibiting human muscarinic acetylcholine 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.
| ln Vitro |
Aclidinium shows strong antagonistic activity against human muscarinic receptors in a preclinical setting. It has a longer half-life at M3 receptors than it does at M2 receptors, indicating that it may have a long-lasting bronchodilator action. Acclidinium hydrolyzes quickly in human plasma, in contrast to tiotropium and other antimuscarinics that are already on the market. Single- and multiple-dose aclidinium has a good safety profile and a low systemic bioavailability, according to early clinical trials conducted in healthy participants. Aclidinium exhibited prolonged bronchodilatory action and was well tolerated in 464 individuals with moderate to severe COPD who participated in a subsequent phase IIb research.
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| ln Vivo |
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| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation Although no published data exist on the use of aclidinium during breastfeeding, it produces low maternal serum levels because of rapid hydrolysis to inactive metabolites. The risk to the breastfed infant of maternal aclidinium inhalation is small. Breastfeeding can be continued during aclidinium therapy. ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. |
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| Additional Infomation |
Aclidinium bromide is a quaternary ammonium salt that is the bromide salt of aclidinium. A muscarinic acetylcholine M3 receptor antagonist, for the long-term maintenance treatment of bronchospasm associated with chronic obstructive pulmonary disease (COPD). It has a role as a muscarinic antagonist and a bronchodilator agent. It is a quaternary ammonium salt and an organic bromide salt. It contains an aclidinium.
See also: Aclidinium (has active moiety); Aclidinium bromide; formoterol fumarate (component of). Drug Indication Eklira Genuair is indicated as a maintenance bronchodilator treatment to relieve symptoms in adult patients with chronic obstructive pulmonary disease (COPD). Bretaris Genuair is indicated as a maintenance bronchodilator treatment to relieve symptoms in adult patients with chronic obstructive pulmonary disease (COPD). |
| Molecular Formula |
C26H30NO4S2.BR
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|---|---|
| Molecular Weight |
564.55
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| Exact Mass |
563.079
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| CAS # |
320345-99-1
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| Related CAS # |
320345-99-1 (bromide);727649-81-2 (cation);
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| PubChem CID |
11519741
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| Appearance |
Off-white to pink solid powder
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| LogP |
1.629
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
34
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| Complexity |
647
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C1C[N+]2(CCC1[C@H](C2)OC(=O)C(C3=CC=CS3)(C4=CC=CS4)O)CCCOC5=CC=CC=C5.[Br-]
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| InChi Key |
XLAKJQPTOJHYDR-QTQXQZBYSA-M
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| InChi Code |
InChI=1S/C26H30NO4S2.BrH/c28-25(26(29,23-9-4-17-32-23)24-10-5-18-33-24)31-22-19-27(14-11-20(22)12-15-27)13-6-16-30-21-7-2-1-3-8-21;/h1-5,7-10,17-18,20,22,29H,6,11-16,19H2;1H/q+1;/p-1/t20?,22-,27?;/m0./s1
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| Chemical Name |
[(3R)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octan-3-yl] 2-hydroxy-2,2-dithiophen-2-ylacetate;bromide
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| Synonyms |
LAS 34273, LAS W 330; LAS-34273, LAS-W 330; LAS34273, LASW 330; trade name: Eklira Genuair; Tudorza Genuair; Bretaris Genuair
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.43 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.43 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.43 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 30% PEG400+0.5% Tween80+5% Propylene glycol : 30 mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7713 mL | 8.8566 mL | 17.7132 mL | |
| 5 mM | 0.3543 mL | 1.7713 mL | 3.5426 mL | |
| 10 mM | 0.1771 mL | 0.8857 mL | 1.7713 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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