Revefenacin

Igoa vaila'au:

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

upu autu:

Revefenacin, TD-4208, GSK-1160724, TD4208, TD 4208, GSK1160724, GSK 1160724, 864750-70-9

Solubility:Solu i le DMSO

Teuina:0 - 4°C mo taimi pupuu (aso i vaiaso), poo le -20°C mo taimi uumi (masina).

Fa'amatalaga:

In Vitro: O le Kis o le revefenacin e 0.42, 0.32, 0.18, 0.56, ma le 6.7 nM i tagata M1, M2, M3, M4 ma M5 faʻafeiloaʻi. I se su'esu'ega fa'atino, o le revefenacin o lo'o fa'aalia o se fa'alavelave fa'atino fa'atasi ai ma fa'alavelave fa'alavelave e pei o le fusifusia o Ki. O le Revefenacin fo'i e fa'alavelaveina le fa'aosoina o le agonist o le fa'amama fa'amama fa'amama fa'atasi ma le fa'atasi o le 0.1 nM, tutusa ma le M3 biding Ki[1]. I totonu o Vivo: I totonu o maile faʻamaʻi, revefenacin, faʻatasi ai ma le tiotropium ma le glycopyrronium, e maua ai le taofiofia tumau o le acetylcholine-induced bronchoconstriction mo le 24 itula. I isumu fa'ama'i, o le revefenacin inhaled o lo'o fa'aalia ai le bronchoprotection 24-itula fa'alagolago i fuala'au fa'asaga i le bronchoconstriction e mafua mai i le methacholine. Ole fua fa'atatau ile 24-itula ole malosi ole 45.0 µg/mL ma ole malosi ole bronchoprotective e fa'atumauina pea pe a uma le 7 aso ole fa'a-tasi i le aso [2].

Sini: mAChR