Revefenacin

Orukọ Kemikali:

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

KỌỌDỌ SMILES:

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

Koodu 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)

Bọtini InChi:

FYDWDCIFZSGNBU-UHFFFAOYSA-N

Koko-ọrọ:

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

Solubility:Tiotuka ni DMSO

Ibi ipamọ:0 - 4°C fun igba kukuru (ọjọ si awọn ọsẹ), tabi -20°C fun igba pipẹ (osu).

Apejuwe:

Ni Vitro: Awọn Kis ti revefenacin jẹ 0.42, 0.32, 0.18, 0.56, ati 6.7 nM ni eniyan M1, M2, M3, M4 ati M5 awọn olugba, lẹsẹsẹ. Ninu ayẹwo iṣẹ-ṣiṣe, revefenacin ni a fihan lati jẹ antagonist ti iṣẹ-ṣiṣe pẹlu awọn idiwọn idinamọ ti o jọra si di Ki's. Revefenacin tun ṣe idiwọ ihamọ ti o fa agonist ti igbaradi oruka tracheal pig ti o ya sọtọ pẹlu isunmọ 0.1 nM, ti o jọra si idiwon M3 biding Ki[1]. Ni Vivo: Ninu awọn aja ti anesthetized, revefenacin, pẹlu tiotropium ati glycopyrronium, gbejade idinamọ idaduro ti bronchoconstriction ti o fa acetylcholine fun wakati 24. Ninu awọn eku anesthetized, ifasimu revefenacin ṣe afihan iwọn lilo-igbẹkẹle 24-wakati bronchoprotection lodi si methacholine-induced bronchoconstriction. Agbara wakati 24 ti a pinnu jẹ 45.0 µg/mL ati pe awọn agbara bronchoprotective ti wa ni itọju lẹhin awọn ọjọ meje ti iwọn lilo lẹẹkan lojoojumọ[2].

afojusun: mAChR