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Synonyms | GW642444M Trifenate | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C24H33Cl2NO5.C20H16O2 |
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分子量 | 774.77 | CAS No. | 503070-58-4 | ||||||||
Solubility (25°C)* | 体外 | DMSO | 100 mg/mL (129.07 mM) | ||||||||
Ethanol | 10 mg/mL (12.9 mM) | ||||||||||
Water | Insoluble | ||||||||||
体内 (毎回新しく調製した物を用意してください) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | Vilanterol trifenatate (GW642444M) is a novel inhaled long-acting beta2 adrenoceptor agonist with inherent 24-hour activity for once daily treatment of COPD and asthma. |
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in vitro | Vilanterol displays a subnanomolar affinity for the β2-AR that is comparable with that of salmeterol but higher than olodaterol, formoterol, and indacaterol. In cAMP functional activity studies, vilanterol demonstrates similar selectivity as salmeterol for β2- over β1-AR and β3-AR, but a significantly improved selectivity profile than formoterol and indacaterol. Vilanterol also shows a level of intrinsic efficacy that is comparable to indacaterol but significantly greater than that of salmeterol. In cellular cAMP production and tissue-based studies measuring persistence and reassertion, vilanterol has a persistence of action comparable with indacaterol and longer than formoterol. In addition, vilanterol demonstrates reassertion activity in both cell and tissue systems that is comparable with salmeterol and indacaterol but longer than formoterol. In human airways, vilanterol is shown to have a faster onset and longer duration of action than salmeterol, exhibiting a significant level of bronchodilation 22 h after treatment[1]. |
Development of 3D-QSAR models for predicting the activities of chemicals to stimulate muscle growth via β2-adrenoceptor [ Toxicol In Vitro, 2021, 77:105251] | PubMed: 34601065 |
Mechanism underlying β2-AR agonist-mediated phenotypic conversion of LPS-activated microglial cells [ J Neuroimmunol, 2019, 332:37-48] | PubMed: 30933849 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。