Revefenacin

Lub npe tshuaj:

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(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- dr hab. 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

Lo lus tseem ceeb:

Tom ntej: Revefenacin TD-4208 GSK-1160724 TD4208 TD 4208 GSK1160724 GSK 1160724 864750-70-9

Solubility:Soluble hauv DMSO

Cia:0 - 4 ° C rau lub sijhawm luv (hnub mus rau lub lis piam), lossis -20 ° C rau lub sijhawm ntev (hli).

Nqe lus piav qhia:

Hauv Vitro: Cov Kis ntawm revefenacin yog 0.42, 0.32, 0.18, 0.56, thiab 6.7 nM ntawm tib neeg M1, M2, M3, M4 thiab M5 receptors, feem. Hauv kev ntsuam xyuas ua haujlwm, revefenacin tau pom tias yog ib qho kev ua haujlwm antagonist nrog inhibition tas li zoo li khi Ki's. Revefenacin kuj inhibits agonist-induced contraction ntawm guinea npua cais tracheal nplhaib npaj nrog affinity ntawm 0.1 nM, zoo ib yam li ntsuas M3 biding Ki[1]. Hauv Vivo: Hauv cov dev uas tau txhaj tshuaj loog, revefenacin, nrog rau tiotropium thiab glycopyrronium, tsim kev cuam tshuam ntawm acetylcholine-induced bronchoconstriction mus txog 24 teev. Hauv cov nas uas muaj tshuaj loog, nqus tau cov tshuaj revefenacin pom cov koob tshuaj 24-teev bronchoprotection tiv thaiv methacholine-induced bronchoconstriction. Qhov kwv yees li ntawm 24-teev potency yog 45.0 µg / mL thiab cov bronchoprotective potencies tau khaws cia tom qab 7 hnub ntawm kev noj ib hnub ib zaug[2].

Hom phiaj: mAChR