All AbMole products are for research use only, cannot be used for human consumption.
Revefenacin (TD-4208; GSK1160724) is a novel long-acting muscarinic antagonist currently in clinical development for the treatment of respiratory diseases, including bronchospasm due to COPD. The purpose of our studies was to characterize the in vivo bronchoprotective and antisialagogue effect of this new agent. In two preclinical species, we showed that inhaled TD-4208 produces sustained bronchoprotective activity up to 24 hours after dosing. Moreover, after 7-day repeat dosing in rats, equieffective bronchoprotective doses of TD-4208 inhibited salivation to a much lesser extent than the other two muscarinic antagonists. Thus, TD-4208 exhibits greater lung selectivity than either tiotropium or glycopyrronium.
| Cell Experiment | |
|---|---|
| Cell lines | CHO-K1 (Chinese hamster ovary-K1) cell lines |
| Preparation method | CHO-K1 (Chinese hamster ovary-K1) cell lines stably expressing hM1, hM3, M4-G16α and cM5 mAChR subtypes, respectively, were grown to near confluency in medium consisting of HAM's F-12 supplemented with 10% FBS and 250 μg mL-1 Geneticin. The chimpanzee M5 receptor was utilized as a surrogate of the human M5 due to intellectual property restrictions surrounding use of the latter in cell-based studies. Cells were gently washed and treated for 40 minutes at 37°C with the membrane permeable, calcium sensitive dye, FLUO-4AM and, following a wash, were then incubated with increasing concentrations of revefenacin for 20 minutes at 37°C. The cells were stimulated with oxotremorine at a concentration required to elicit 90% of the maximal response (EC90). The change in fluorescence was measured using a FLIPR®-Tetra. |
| Concentrations | |
| Incubation time | 20 minutes |
| Animal Experiment | |
|---|---|
| Animal models | Dogs |
| Formulation | |
| Dosages | 3, 10, and 30 µg/kg |
| Administration | i.v. |
| Molecular Weight | 597.75 |
| Formula | C35H43N5O4 |
| CAS Number | 864750-70-9 |
| Form | Solid |
| Solubility (25°C) | DMSO 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related AChR/AChE Products |
|---|
| VU 0255035
VU 0255035 is a highly selective M1 muscarinic acetylcholine receptor (mAChR) antagonist (Ki = 14.87 nM). |
| Fesoterodine fumarate
Fesoterodine fumarate (Toviaz) is a novel muscarinic receptor antagonist. |
| SVT-40776
SVT-40776 is a novel M3 muscarinic receptor antagonist. |
| Aniracetam
Aniracetam is a compound that promotes intellectual development and neuroprotection. |
| Biperiden hydrochloride
Biperiden (KL 373) hydrochloride is a non-selective muscarinic receptor antagonist that competitively binds to M1 muscarinic receptors, thereby inhibiting acetylcholine and enhancing dopamine signaling in the central nervous system. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2026 AbMole BioScience. All Rights Reserved.
