Revefenacin

Lebitso la lik'hemik'hale:

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

SMILES Khouto:

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

Khoutu ea InChi:

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

Sollubility:E qhibiliha ka DMSO

Polokelo:0 - 4 ° C bakeng sa nako e khutšoanyane (matsatsi ho isa libeke), kapa -20 ° C bakeng sa nako e telele (likhoeli).

Tlhaloso:

In Vitro: Kis ea revefenacin ke 0.42, 0.32, 0.18, 0.56, le 6.7 nM ho batho ba M1, M2, M3, M4 le M5 receptors, ka ho latellana. Tekong ea ts'ebetso, revefenacin e bonts'oa e le mohanyetsi ea sebetsang ea nang le li-inhibition constants tse ts'oanang le ho tlama Ki's. Revefenacin e boetse e thibela khohlano e bakoang ke agonist ea ho itokisa ha lesale la tracheal le le leng le nang le kamano ea 0.1 nM, e tšoanang le ea M3 biding Ki[1] e lekantsoeng. Ho Vivo: Lintjang tse hlabosang, revefenacin, hammoho le tiotropium le glycopyrronium, li hlahisa thibelo e tsitsitseng ea acetylcholine-induced bronchoconstriction ho fihlela lihora tse 24. Likhotong tse nang le li-anesthetized, revefenacin e hemang e bonts'a ts'ireletso ea lihora tse 24 ea bronchoprotection khahlanong le methacholine-induced bronchoconstriction. Ho hakanngoa hore matla a lihora tse 24 ke 45.0 µg/mL 'me matla a bronchoprotective a bolokoa ka mor'a matsatsi a 7 a ho noa hanngoe ka letsatsi[2].

Sepheo: mAChR