Revefenacin
Product Detail
Product Tags
Pack Size | Availability | Price (USD) |
10mg | In stock | 200 |
100mg | In stock | 800 |
1g | In stock | 3400 |
More Sizes | Get Quotes | Get Quotes |
Chemical Name:
1-(2-(3-((4-carbamoylpiperidin-1-yl)methyl)-N-methylbenzamido)ethyl)piperidin-4-yl [1,1'-biphenyl]-2-ylcarbamate
SMILES Code:
O=C(OC1CCN(CCN(C)C(C2=CC=C(CN3CCC(C(N)=O)CC3)C=C2)=O)CC1)NC4=CC=CC=C4C5=CC=CC=C5
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)
InChi Key:
FYDWDCIFZSGNBU-UHFFFAOYSA-N
Keyword:
Revefenacin, TD-4208, GSK-1160724, TD4208, TD 4208, GSK1160724, GSK 1160724, 864750-70-9
Solubility: Soluble in DMSO
Storage: 0 - 4°C for short term (days to weeks), or -20°C for long term (months).
Description:
In Vitro:The Kis of revefenacin are 0.42, 0.32, 0.18, 0.56, and 6.7 nM at human M1, M2, M3, M4 and M5 receptors, respectively. In a functional assay, revefenacin is shown to be a functional antagonist with inhibition constants similar to binding Ki's. Revefenacin also inhibits agonist-induced contraction of guinea pig isolated tracheal ring preparation with an affinity of 0.1 nM, similar to the measured M3 biding Ki[1]. In Vivo:In anesthetized dogs, revefenacin, along with tiotropium and glycopyrronium, produce sustained inhibition of acetylcholine-induced bronchoconstriction for up to 24 hours. In anesthetized rats, inhaled revefenacin exhibits dose-dependent 24-hour bronchoprotection against methacholine-induced bronchoconstriction. The estimated 24-hour potency is 45.0 µg/mL and the bronchoprotective potencies are maintained after 7 days of once-daily dosing[2].
Target: mAChR