Protein Agonists, Antagonists and Activators - Batefenterol (CAS: 743461-65-6)

Batefenterol (CAS: 743461-65-6)

Catalog #：EBC51037

Biological Activity

Synonyms

GSK961081, TD-5959

Chemical Name

(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

Application

Batefenterol is a muscarinic receptor antagonist and β2-adrenoceptor agonist

CAS Number

743461-65-6

Purity

≥98.0%

Molecular Weight

740.24

Molecular Formula

C₄₀H₄₂ClN₅O₇

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

Target & IC50

hβ2-adrenoceptor agonist: EC50 = 0.29 nM

Shipping

Gel Pack

Storage

Store at -20°C

Preparing Stock Solutions

Molecular Structure

ConcentrationSolventMass	1 mg	5 mg	10 mg
1 mM	1.3509 ml	6.7545 ml	13.5091 ml
5 mM	0.2702 ml	1.3509 ml	2.7018 ml
10 mM	0.1351 ml	0.6755 ml	1.3509 ml
50 mM	0.0270 ml	0.1351 ml	0.2702 ml

Solubility
DMSO: 100 mg/mL (135.09 mM)

Product Description

Batefenterol is a Muscarinic Antagonist and β2-Agonist possessing both muscarinic antagonist (MA) and β2-adrenoceptor agonist (BA) properties (MABA). GSK-961081 displayed high affinity for hM2 (Ki = 1.4 nM), hM3 muscarinic receptors (Ki = 1.3 nM) and hβ2-adrenoceptors (Ki = 3.7 nM). GSK-961081 behaved as a potent hβ2-adrenoceptor agonist (EC50 = 0.29 nM for stimulation of cAMP levels) with 440- and 320-fold functional selectivity over hβ1- and hβ3-adrenoceptors, respectively.