I-Batefenterol

Igama Lekhemikhali:

"(R)-1-(3-((2-chloro-4-(((2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethyl)amino) methyl)-5-methoxyphenyl)amino)-3-oxopropyl)piperidin-4-yl [1,1'-biphenyl]-2-ylcarbamate Batefenterol Succinate"

Ikhodi ye-SMILES:

O=C(OC1CCN(CCC(NC2=CC(OC)=C(CNC[C@H](O)C3=CC=C(O)C4=C3C=CC(N4)=O)C=C2Cl)= O)CC1)NC5=CC=CC=C5C6=CC=CC=C6

Ikhodi ye-InChi:

I-InChI=1S/C40H42ClN5O7/c1-52-36-22-33(31(41)21-26(36)23-42-24-35(48)29-11-13-34(47)39-30( 29)12-14-37(49)45-39)43-38(50)17-20-46-18-15-27(16-19-46)53-40(51)44-32-10- 6-5-9-28(32)25-7-3-2-4-8-25/h2-14,21-22,27,35,42,47-48H,15-20,23-24H2, 1H3,(H,43,50)(H,44,51)(H,45,49)/t35-/m0/s1

I-InChi Key:

URWYQGVSPQJGGB-DHUJRADRSA-N

Igama elingukhiye:

Batefenterol, TD-5959, GSK961081, 743461-65-6, GSK-961081, GSK 961081, TD5959, TD 5959, 743461-65-6

Ukunyibilika:I-Soluble ku-DMSO

Isitoreji:0 - 4°C isikhathi esifushane (izinsuku ukuya emavikini), noma -20°C isikhathi eside (izinyanga)

Incazelo:

I-Batefenterol iyi-antagonist ye-muscarinic kanye ne-β2-adrenergic receptor (β2-AR) agonist (Kis = 1.4, 1.3, kanye ne-3.7 nM, ye-hM2, hM3, ne-hβ2-AR, ngokulandelanayo ku-assay ebopha i-radioligand). I-Batefenterol ibonisa umsebenzi we-agonist onamandla we-hβ2-AR (EC50 = 0.29 nM) ngokukhetha okusebenzayo okungu-440- kanye ne-320-fold phezu kwe-hβ1- kanye ne-hβ3-ARs, ngokulandelana.1 I-Batefenterol yenza ukuphumula kwemisipha ebushelelezi (EC50 = 11 nM) ku-tracheal Guinea eyedwa izicubu futhi ivimbela impendulo ye-bronchoconstrictor ku-guinea pig bronchoprotection assay (ED50 = 6.4 µg/mL). Amafomula aqukethe i-batefenterol asezivivinyweni zomtholampilo zokwelapha isifo esingamahlalakhona sokuvimbela i-pulmonary (COPD).

Ithagethi: β2-adrenoceptor