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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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Purity: ≥98%
Vilanterol trifenatate (formerly GW-642444; Anoro Ellipta; Breo Ellipta), the trifenatate salt of vilanterol, is an ultra-long-acting β2-adrenoceptor/ beta-2 (β2-AR) agonist approved in May 2013 for use in combination with fluticasone furoate (Breo Ellipta) and also in combination with Umeclidinium bromide (Anoro Ellipta) for the treatment of chronic obstructive pulmonary disease (COPD).The pEC50 values for β2-AR, β1-AR, and β3-AR are 10.37±0.05, 6.98±0.03, and 7.36±0.03, in that order.
Targets |
β2-adrenoceptor
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ln Vitro |
Vilanterol exhibits a subnanomolar affinity for the β2-AR that is greater than that of olodaterol, formoterol, and indacaterol, but similar to salmeterol's. Vilanterol shows comparable selectivity to salmeterol for β2-over β1-AR and β3-AR in cAMP functional activity studies, but a markedly better selectivity profile than formoterol and indacaterol. Additionally, vilanterol exhibits an intrinsic efficacy that is notably higher than salmeterol but comparable to indacaterol. Vilanterol exhibits a longer duration of action than formoterol and a persistence of action similar to indacaterol in tissue-based studies measuring persistence and reassertion and cellular cAMP production. Furthermore, vilanterol exhibits reassertion activity in tissue and cell systems that is longer than formoterol but comparable to salmeterol and indacaterol. Vilanterol has been demonstrated to exhibit a significant degree of bronchodilation 22 hours after treatment, with a faster onset and longer duration of action in human airways than salmeterol[1].
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References |
Molecular Formula |
C44H49CL2NO
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Molecular Weight |
774.76836
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Exact Mass |
485.17
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Elemental Analysis |
C, 68.21; H, 6.38; Cl, 9.15; N, 1.81; O, 14.45
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CAS # |
503070-58-4
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Related CAS # |
Vilanterol; 503068-34-6; Vilanterol-d4 trifenatate; 2021249-10-3; 503070-58-4 (trifenatate)
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Appearance |
Solid powder
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SMILES |
C1=CC=C(C=C1)C(C2=CC=CC=C2)(C3=CC=CC=C3)C(=O)O.C1=CC(=C(C(=C1)Cl)COCCOCCCCCCNC[C@@H](C2=CC(=C(C=C2)O)CO)O)Cl
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InChi Key |
KLOLZALDXGTNQE-JIDHJSLPSA-N
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InChi Code |
InChI=1S/C24H33Cl2NO5.C20H16O2/c25-21-6-5-7-22(26)20(21)17-32-13-12-31-11-4-2-1-3-10-27-15-24(30)18-8-9-23(29)19(14-18)16-28;21-19(22)20(16-10-4-1-5-11-16,17-12-6-2-7-13-17)18-14-8-3-9-15-18/h5-9,14,24,27-30H,1-4,10-13,15-17H2;1-15H,(H,21,22)/t24-;/m0./s1
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Chemical Name |
4-[(1R)-2-[6-[2-[(2,6-dichlorophenyl)methoxy]ethoxy]hexylamino]-1-hydroxyethyl]-2-(hydroxymethyl)phenol;2,2,2-triphenylacetic acid
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Synonyms |
GW-642444; GW 642444-X; GW 642444 X; GW642444; GW-642444; GW 642444X; Anoro Ellipta; Breo Ellipta
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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) |
DMSO: 50~100 mg/mL (64.5~129.1 mM)
Ethanol: ~14 mg/mL |
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Solubility (In Vivo) |
Solubility in Formulation 1: 2 mg/mL (2.58 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 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 mg/mL (2.58 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 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 mg/mL (2.58 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.2907 mL | 6.4535 mL | 12.9071 mL | |
5 mM | 0.2581 mL | 1.2907 mL | 2.5814 mL | |
10 mM | 0.1291 mL | 0.6454 mL | 1.2907 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.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT01498679 | Completed | Drug: GW685698/GW642444 (fluticasone furoate/vilanterol trifenatate) |
Asthma | GlaxoSmithKline | January 2012 | Phase 3 |
NCT03184987 | Completed | Drug: FF/UMEC/VI 100/62.5/25 mcg Drug: FF/UMEC/VI 200/62.5/25 mcg Drug: Salbutamol |
Asthma | GlaxoSmithKline | June 22, 2017 | Phase 3 |
NCT05062304 | Completed | Drug: Vicriviroc maleate Drug: Placebo |
HIV Infections | Merck Sharp & Dohme LLC | July 2007 | N/A |
NCT03739294 | Completed | Drug: Fluticasone Furoate/ Vilanterol Trifenatate |
Pharmacokinetics | Bispebjerg Hospital | February 8, 2019 | Phase 2 |
NCT01498653 | Completed | Drug: GW685698/GW642444 Drug: CCI18781 |
Asthma | GlaxoSmithKline | January 2012 | Phase 3 |