Batefenterol (GSK961081;TD-5959)是一种新的muscarinic受体拮抗剂和β₂-肾上腺素受体激动剂; 对hM2，hM3和β₂-肾上腺素受体有高亲和力，K_i值分别为1.4, 1.3和3.7nM。

Batefenterol (GSK961081;TD-5959) is a novel muscarinic receptor antagonist and β 2 -adrenoceptor agonist; displays high affinity for hM2, hM3 muscarinic and hβ 2 -adrenoceptor with K i values of 1.4, 1.3 and 3.7 nM, respectively.

Solid

mAChR2 mAChR3

Batefenterol is a novel first-in-class inhaled bifunctional compound possessing both muscarinic antagonist (MA) and β2-adrenoceptor agonist (BA) properties (MABA). In competition radioligand binding studies at human recombinant receptors, batefenterol displays high affinity for hM2 (Ki=1.4 nM), hM3 muscarinic receptors (Ki=1.3 nM) and hβ2-adrenoceptors (Ki=3.7 nM). Batefenterol behaves 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. has not independently confirmed the accuracy of these methods. They are for reference only.

In the guinea pig bronchoprotection assay, inhaled Batefenterol produces potent, dose-dependent inhibition of bronchoconstrictor responses via MA (ED 50 =33.9 μg/mL), BA (ED 50 =14.1 μg/mL), and MABA (ED 50 =6.4 μg/mL) mechanisms. Significant bronchoprotective effects of Batefenterol are evident in guinea pigs via MA, BA, and MABA mechanisms for up to 7 days after dosing. In guinea pig isolated trachea expressing native muscarinic M3 and β 2 , batefenterol produces smooth muscle relaxation through a dual mechanism involving competitive antagonism of the M3 receptor (EC 50 =50 nM) and agonism of the β 2 receptor (EC 50 =25 nM). The combined effect on both muscarinic receptors and β 2 receptors is more potent than either function working alone (EC 50 =10 nM). Batefenterol exhibits a rapid rate of

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Hegde SS, et al. Pharmacologic characterization of GSK-961081 (TD-5959), a first-in-class inhaled bifunctional bronchodilator possessing muscarinic receptor antagonist and β2-adrenoceptor agonist properties. J Pharmacol Exp Ther. 2014 Oct;351(1):190-9.
[2]. Hughes AD, et al. Discovery of (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 (TD-5959, GSK961081, batefenterol): first-in-class dual pharmacology multivalent muscarinic anta

In Vitro: DMSO : ≥ 100 mg/mL (135.09 mM)配制储备液