Revefenacin

Igama leMchiza:

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

Ikhowudi yoncumo:

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

Ikhowudi ye-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)

Isitshixo se-InChi:

FYDWDCIFZSGNBU-UHFFFAOYSA-N

Igama elingundoqo:

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

Ukunyibilika:Inyibilika kwi-DMSO

Ugcino:0 - 4°C ixesha elifutshane (iintsuku ukuya kwiiveki), okanye -20°C ixesha elide (iinyanga).

Inkcazo:

Kwi-Vitro: I-Kis ye-revefenacin yi-0.42, 0.32, 0.18, 0.56, kunye ne-6.7 nM kwi-M1 yabantu, i-M2, i-M3, i-M4 kunye ne-M5 receptors, ngokulandelanayo. Kwi-assay esebenzayo, i-revefenacin iboniswa ukuba ngumchasi osebenzayo kunye ne-inhibition constants efana nokubopha i-Ki. I-Revefenacin iphinda inqanda ukunyanzeliswa kwe-agonist-induced contraction ye-guinea pig isolated ring ye-tracheal ring kunye ne-affinity ye-0.1 nM, efana ne-M3 ye-biding ye-Ki[1]. Kwi-Vivo: Kwizinja ezine-anesthetized, i-revefenacin, kunye ne-tiotropium kunye ne-glycopyrronium, ivelisa isithintelo esiqhubekayo se-acetylcholine-induced bronchoconstriction ukuya kwiiyure ezingama-24. Kwiimpuku ezifakwe i-anesthetized, i-revefenacin ephefumleyo ibonisa i-24 yeyure exhomekeke kwi-bronchoprotection ngokuchasene ne-methacholine-induced bronchoconstriction. Uqikelelo lweeyure ze-24 potency yi-45.0 µg / mL kwaye amandla e-bronchoprotective agcinwa emva kweentsuku ze-7 ze-dosing kanye ngosuku [2].

Ithagethi: mAChR