ʻO Revefenacin

Inoa Kimia:

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(C(N)=O)CC3)C=C2)=O)CC1)NC4=CC=CC=C4C5=CC=CC= C5

Code 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)

Ki InChi:

FYDWDCIFZSGNBU-UHFFFAOYSA-N

huaʻōlelo:

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

Hiki ke hoʻoheheʻe:Hiki ke hoʻoheheʻe ʻia ma DMSO

Waihona:0 - 4°C no ka wā pōkole (nā lā i nā pule), a i ʻole -20°C no ka wā lōʻihi (mau mahina).

wehewehe:

In Vitro: ʻO ka Kis o revefenacin he 0.42, 0.32, 0.18, 0.56, a me 6.7 nM ma nā mea hoʻokipa M1, M2, M3, M4 a me M5. I loko o kahi ho'āʻo hana, hōʻike ʻia ʻo revefenacin he mea kū'ē i ka hana me nā mea paʻa paʻa e like me ka hoʻopaʻa ʻana iā Ki. Hoʻopaʻa pū ʻo Revefenacin i ka agonist-induced contraction o ka puaʻa guinea i hoʻokaʻawale i ka hoʻomākaukau ʻana i ke apo tracheal me kahi pili o 0.1 nM, e like me ke ana ʻana i ka M3 biding Ki[1]. In Vivo：Ma nā ʻīlio hoʻomaʻamaʻa, ʻo revefenacin, me ka tiotropium a me ka glycopyrronium, hana i ka pale mau ʻana o ka acetylcholine-induced bronchoconstriction a hiki i 24 mau hola. I nā ʻiole hoʻomaʻemaʻe, hōʻike ka revefenacin inhaled i ka bronchoprotection 24-hola e pili ana i ka methacholine-induced bronchoconstriction. ʻO ka mana o 24 mau hola he 45.0 µg / mL a mālama ʻia nā mana bronchoprotective ma hope o 7 mau lā o ka hoʻohana ʻana i hoʻokahi lā.

Kuhikuhi: mAChR