A muscarinic antagonist and β2-adrenergic receptor (β2-AR) agonist (Kis = 1.4

Batefenterol – 5 mg

Brand:
Cayman
CAS:
743461-65-6
Storage:
-20
UN-No:
Non-Hazardous - /

Batefenterol is a muscarinic antagonist and β2-adrenergic receptor (β2-AR) agonist (Kis = 1.4, 1.3, and 3.7 nM, for hM2, hM3, and hβ2-AR, respectively in a radioligand binding assay).{40016, 40017} Batefenterol exhibits potent hβ2-AR agonist activity (EC50 = 0.29 nM) with 440- and 320-fold functional selectivity over hβ1- and hβ3-ARs, respectively.{40016} Batefenterol induces smooth muscle relaxation (EC50 = 11 nM) in isolated guinea pig tracheal tissue and inhibits bronchoconstrictor response in a guinea pig bronchoprotection assay (ED50 = 6.4 µg/ml).{40016} Formulations containing batefenterol are in clinical trials to treat chronic obstructive pulmonary disease (COPD).{40018}  

 

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Description

A muscarinic antagonist and β2-adrenergic receptor (β2-AR) agonist (Kis = 1.4, 1.3, and 3.7 nM, for hM2, hM3, and hβ2-AR, respectively); exhibits potent hβ2-AR agonist activity (EC50 = 0.29 nM) with 440- and 320-fold selectivity over hβ1- and hβ3-ARs, respectively; induces smooth muscle relaxation; inhibits bronchoconstrictor response

Formal name: N-[1,1′-biphenyl]-2-yl-carbamic acid, 1-[3-[[2-chloro-4-[[[(2R)-2-(1,2-dihydro-8-hydroxy-2-oxo-5-quinolinyl)-2-hydroxyethyl]amino]methyl]-5-methoxyphenyl]amino]-3-oxopropyl]-4-piperidinyl ester

Synonyms:  GSK961081|TD-5959

Molecular weight: 740.2

CAS: 743461-65-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Immunology & Inflammation|Pulmonary Diseases|COPD/Emphysema

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