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| 25mg |
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Purity: ≥98%
Revefenacin (formerly known as TD-4208; GSK-1160724; trade name: Yupelri) is a long-acting, potent mAChR (muscarinic acetylcholine receptor) antagonist with a high affinity on M3 receptor with a Ki of 0.18 nM. It may be applied in the management of respiratory conditions. The FDA approved revefenacin on November 8, 2018, for the treatment of patients with chronic obstructive pulmonary disease (COPD). Prior to this, Tiotropium was the only once-daily long-acting muscarinic antagonist (LAMA) that was authorized for the treatment of COPD in the US and other nations. Recently, the European Union approved glycopyrronium as a once-daily maintenance treatment for COPD, based on its promising performance as a LAMA. In summary, revefenacin may be used once daily to treat respiratory disorders as a long-acting bronchodilator. In comparison to commercially available muscarinic receptor antagonists, it may have a better tolerability profile due to its increased functional selectivity for the lung in preclinical models.
| Targets |
M1 ( Ki = 0.42 nM ); M2 ( Ki = 0.32 nM ); M3 ( Ki = 0.18 nM ); M4 ( Ki = 0.56 nM ); M5 ( Ki = 6.7 nM )
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| ln Vivo |
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| Animal Protocol |
Rats: Rats are exposed by inhaling a nebulized solution of either vehicle (sterile water) or revefenacin (3–3000 µg/mL), tiotropium (0.3–300 µg/mL), or glycopyrronium (1–1000 µg/mL) to ascertain the bronchoprotective and antisialagogue potency after a single dose. 24 hours after the dosage, bronchoprotective activity is evaluated. The antisialagogue effect's peak effect time is determined by measuring the inhibition of Pilo 1, 6, or 12 hours after an effective dose of the test compound was inhaled. At this point in time, all subsequent doses are measured[2].
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| References |
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| Molecular Formula |
C35H43N5O4
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| Molecular Weight |
597.76
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| Exact Mass |
597.33
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| Elemental Analysis |
C, 70.33; H, 7.25; N, 11.72; O, 10.71
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| CAS # |
864750-70-9
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| Related CAS # |
864750-70-9; 864751-51-9 (phosphate); 864751-53-1 (sulfate); 864751-55-3 (oxalate)
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| Appearance |
Solid powder
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| SMILES |
CN(CCN1CCC(CC1)OC(=O)NC2=CC=CC=C2C3=CC=CC=C3)C(=O)C4=CC=C(C=C4)CN5CCC(CC5)C(=O)N
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| InChi Key |
FYDWDCIFZSGNBU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C35H43N5O4/c1-38(34(42)29-13-11-26(12-14-29)25-40-19-15-28(16-20-40)33(36)41)23-24-39-21-17-30(18-22-39)44-35(43)37-32-10-6-5-9-31(32)27-7-3-2-4-8-27/h2-14,28,30H,15-25H2,1H3,(H2,36,41)(H,37,43)
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| Chemical Name |
[1-[2-[[4-[(4-carbamoylpiperidin-1-yl)methyl]benzoyl]-methylamino]ethyl]piperidin-4-yl] N-(2-phenylphenyl)carbamate
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| Synonyms |
TD-4208; TD4208; GSK-1160724; GSK-1160724; TD 4208; GSK1160724; trade name: Yupelri; TD-4208; GSK 1160724
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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 |
| 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 (4.18 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 (4.18 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 (4.18 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6729 mL | 8.3646 mL | 16.7291 mL | |
| 5 mM | 0.3346 mL | 1.6729 mL | 3.3458 mL | |
| 10 mM | 0.1673 mL | 0.8365 mL | 1.6729 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 |
| NCT04315558 | Recruiting | Drug: Ipratropium Bromide Drug: Revefenacin Inhalation Solution [Yupelri] |
COPD Acute Respiratory Failure |
University of California, Los Angeles |
November 1, 2020 | Phase 2 |
| NCT04655170 | Recruiting | Drug: Revefenacin (YUPELRI) & Formoterol (Perforomist) |
COPD Exacerbation | University of Tennessee Graduate School of Medicine |
December 9, 2020 | Phase 4 |
| NCT03573817 | Completed | Drug: Revefenacin Drug: Placebo |
Chronic Obstructive Pulmonary Disease (COPD) |
Mylan Inc. | May 31, 2018 | Phase 3 |
| NCT05165485 | Completed | Drug: Revefenacin Drug: Tiotropium |
Chronic Obstructive Pulmonary Disease (COPD) |
Theravance Biopharma | January 7, 2022 | Phase 4 |
| NCT03095456 | Recruiting | Drug: Revefenacin Drug: Placebo for Revefenacin |
Low Peak Inspiratory Flow Rate (PIFR) |
Mylan Inc. | March 27, 2017 | Phase 3 |
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