Revefenacin

Dzina la Chemical:

1-(2-(3-((4-carbamoylpiperidin-1-yl)methyl)-N-methylbenzamido)ethyl)piperidin-4-yl [1,1'-biphenyl]-2-ylcarbamate

SMILES Kodi:

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 kodi:

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

Mawu ofunika:

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

Kusungunuka:Zosungunuka mu DMSO

Posungira:0 - 4 ° C kwa nthawi yochepa (masiku mpaka masabata), kapena -20 ° C kwa nthawi yaitali (miyezi).

Kufotokozera:

Mu Vitro: The Kis of revefenacin ndi 0.42, 0.32, 0.18, 0.56, ndi 6.7 nM pa anthu M1, M2, M3, M4 ndi M5 zolandilira. Pakuyesa kogwira ntchito, revefenacin ikuwoneka ngati yolimbana ndi zoletsa zoletsa zofanana ndi zomanga za Ki. Revefenacin imalepheretsanso kugwedezeka kopangidwa ndi agonist kwa kusungunula kwa mphete ya mphira yomwe ili ndi 0.1 nM, yofanana ndi M3 biding Ki[1]. Mu Vivo: Mwa agalu ogonetsa, revefenacin, pamodzi ndi tiotropium ndi glycopyrronium, amatulutsa kuletsa kwa acetylcholine-induced bronchoconstriction kwa maola 24. Mu makoswe ogonetsa, revefenacin wokometsedwa amawonetsa chitetezo cha maola 24 cha bronchoprotection motsutsana ndi methacholine-induced bronchoconstriction. Kuyerekeza kwa maola 24 ndi 45.0 µg/mL ndipo mphamvu za bronchoprotective zimasungidwa pakadutsa masiku 7 akumwa kamodzi patsiku[2].

Zolinga: mAChR