產(chǎn)品目錄

規(guī)格	5mg 10mg 50mg 100mg
CAS	743461-65-6
別名	N/A
化學(xué)名	N/A
分子式	C40H42ClN5O7
分子量	740.24
溶解度	DMSO : ≥ 100 mg/mL (135.09 mM);H2O : < 0.1 mg/mL (insoluble)
儲存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

Batefenterol (GSK961081;TD-5959) is a novel muscarinic receptor antagonist and β2-adrenoceptor agonist; displays high affinity for hM2, hM3 muscarinic and hβ2-adrenoceptor with Ki values of 1.4, 1.3 and 3.7 nM, respectively.

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[1].

In the guinea pig bronchoprotection assay, inhaled Batefenterol produces potent, dose-dependent inhibition of bronchoconstrictor responses via MA (ED50=33.9 μg/mL), BA (ED50=14.1 μg/mL), and MABA (ED50=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[1]. In guinea pig isolated trachea expressing native muscarinic M3 and β2, batefenterol produces smooth muscle relaxation through a dual mechanism involving competitive antagonism of the M3 receptor (EC50=50 nM) and agonism of the β2 receptor (EC50=25 nM). The combined effect on both muscarinic receptors and β2 receptors is more potent than either function working alone (EC50=10 nM). Batefenterol exhibits a rapid rate of clearance and short half-life[2].

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1. 本產(chǎn)品僅供科研使用。請勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請勿存放于普通住宅區(qū)。

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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