Revefenacin - CAS 864750-70-9
Catalog number: B0084-470939
Category: Inhibitor
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Revefenacin, also knownc as TD-4208 and GSK1160724, is potent and selective muscarinic receptor antagonist in development for the treatment of COPD.
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Catalog Number Size Price Stock Quantity
B0084-470939 5 mg $149 In stock
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Solid Powder
TD-4208; TD4208; TD 4208; GSK1160724; GSK-1160724; GSK 1160724
Soluble in DMSO, not in water
Dry, dark and at 0 - 4 ℃ for short term (days to weeks) or -20 ℃ for long term (months to years).
Shelf Life:
2 years
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1.Pharmacological properties of revefenacin (TD-4208), a novel, nebulized long-acting, and lung selective muscarinic antagonist, at human recombinant muscarinic receptors and in rat, guinea pig, and human isolated airway tissues.
Hegde SS;Pulido-Rios MT;Luttmann MA;Foley JJ;Hunsberger GE;Steinfeld T;Lee T;Ji Y;Mammen MM;Jasper JR Pharmacol Res Perspect. 2018 Apr 30;6(3):e00400. doi: 10.1002/prp2.400. eCollection 2018 Jun.
Revefenacin (TD-4208) is a novel, long-acting, and lung-selective muscarinic cholinergic receptor (mAChR) antagonist in development as a nebulized inhalation solution for the treatment of chronic obstructive pulmonary disease (COPD) patients. This study evaluated the pharmacology of revefenacin at human recombinant mAChRs and in airway tissues from rats, guinea pigs, and humans. At human recombinant mAChRs, revefenacin displayed high affinity (pK;I; = 8.2-9.8) and behaved as a competitive antagonist (pKI, apparent = 9.4-10.9) at the five human recombinant mAChRs. Kinetic studies demonstrated that revefenacin dissociated significantly slower from the hM;3; (;t;1/2; = 82 minutes) compared to the hM ;2; (;t;1/2; = 6.9 minutes) mAChR at 37°C, thereby making it kinetically selective for the former subtype. Similarly, in functional studies, revefenacin-mediated antagonism of acetylcholine (ACh)-evoked calcium mobilization responses were reversed less rapidly at hM;3; compared to the hM;2; mAChR. In isolated tracheal tissues from rat and guinea pig and isolated bronchial tissues from humans, revefenacin potently antagonized mAChR-mediated contractile responses. Furthermore, the antagonistic effects of revefenacin in rat, guinea pig, and human airway tissues were slowly reversible (;t;1/2; of 13.
2.Long-acting muscarinic receptor antagonists for the treatment of respiratory disease.
Cazzola M;Page C;Matera MG Pulm Pharmacol Ther. 2013 Jun;26(3):307-17. doi: 10.1016/j.pupt.2012.12.006. Epub 2012 Dec 27.
The use of muscarinic receptor antagonists in the treatment of chronic obstructive pulmonary disease (COPD) is well established. More recently, the potential for long-acting muscarinic receptor antagonists (LAMAs) in the treatment of asthma has also been investigated. While LAMAs offer advantages over short-acting muscarinic receptor antagonists, in terms of a reduced dosing frequency, there remains a need for therapies that improve symptom control throughout both the day and night, provide better management of exacerbations and deliver improved health-related quality of life. Furthermore, the potential for unwanted anticholinergic side effects, particularly cardiovascular effects, remains a concern for this class of compounds. Novel LAMAs in clinical development for the treatment of respiratory disease include: aclidinium bromide, NVA237 (glycopyrronium bromide), GP-MDI, EP-101, CHF-5259, umeclidinium bromide, CHF-5407, TD-4208, AZD8683 and V-0162. These compounds offer potential advantages in terms of onset of action, symptom control and safety. In addition, a number of LAMAs are also being developed as combination treatments with long-acting β2-agonists (LABAs) or inhaled glucocorticosteroids, potentially important treatment options for patients who require combination therapy to achieve an optimal therapeutic response as their disease progresses.
3.Long acting muscarinic antagonists for the treatment of chronic obstructive pulmonary disease: a review of current and developing drugs.
Mastrodicasa MA;Droege CA;Mulhall AM;Ernst NE;Panos RJ;Zafar MA Expert Opin Investig Drugs. 2017 Feb;26(2):161-174. doi: 10.1080/13543784.2017.1276167. Epub 2017 Jan 9.
Long acting muscarinic receptor antagonists (LAMA) reverse airflow obstruction by antagonizing para-sympathetic bronchoconstricting effects within the airways. For years, tiotropium, has been the cornerstone LAMA for chronic obstructive pulmonary disease (COPD) management. Recently, new agents, aclidinium bromide, glycopyrronium bromide, and umeclidinium bromide, have been developed and introduced into clinical practice. Areas covered: This article reviews the clinical efficacy and adverse effects of currently available LAMAs in COPD treatment as well as developing LAMAs in early clinical trials and preclinical studies (V0162, TD-4208, CHF 5407, AZD9164, AZD8683, bencycloquidium). In addition, a new class of molecule that combines muscarinic antagonist and β2-adrenergic properties (MABA) is described and current developmental progress discussed (GSK-961081, THRX-200495). Expert opinion: Future key areas for developing drugs for the management of COPD include prolonged duration of action, optimal delivery systems, synergistic combinations with other drugs, maximization of benefits and minimization of adverse effects. The development of new LAMA and MABA molecules provides exciting progress towards simpler and more effective COPD management.
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CAS 864750-70-9 Revefenacin

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