产品
编 号：F371177
分子式：C24H33Cl2NO5
分子量：486.43
分子式：C24H33Cl2NO5
分子量：486.43
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
50mg
询价
询价
100mg
询价
询价
结构图
CAS No: 503068-34-6
产品详情
生物活性：
Vilanterol (GW642444) is a long-acting β2-adrenoceptor (β2-AR) agonist with 24 h activity. The pEC50s for β2-AR,β1-AR and β3-AR is 10.37±0.05, 6.98±0.03 and 7.36±0.03, respectively.
体外研究：
The selectivity of Vilanterol for β2-AR over the other β-AR receptor subtypes (β2 and β3) is established by testing the ability of Vilanterol to elicit concentration-dependent increases in cAMP in CHO cells expressing human β1-, β2-, and β3-AR. Vilanterol is demonstrated to be highly selective for the β2-AR with at least a 1000-fold selectivity over both β2- and β3-AR subtypes. This analysis results in a low-affinity pKD for [3H]Vilanterol of 9.44±0.07 (n=4) in the presence Gpp(NH)p and a high-affinity pKD of 10.82±0.12 (n=4) and a low-affinity pKD 9.47±0.17 (n=4) in the absence of Gpp(NH)p. In addition, a low-affinity pKD for [3H]Vilanterol of 9.52±0.24 (n=4) in the absence of Gpp(NH)p (37°C) is observed. Vilanterol trifenatate is a novel inhaled long-acting β2-agonist with inherent 24 h activity in vitro in development as a combination with the inhaled corticosteroid fluticasone furoate for both COPD and asthma. Vilanterol is a novel long-acting β2-agonist (LABA) with inherent 24-hour activity for once-daily clinical treatment of chronic obstructive pulmonary disease (COPD) and asthma in combination with the inhaled novel corticosteroid fluticasone furoate, also active for 24 hours.
Vilanterol (GW642444) is a long-acting β2-adrenoceptor (β2-AR) agonist with 24 h activity. The pEC50s for β2-AR,β1-AR and β3-AR is 10.37±0.05, 6.98±0.03 and 7.36±0.03, respectively.
体外研究：
The selectivity of Vilanterol for β2-AR over the other β-AR receptor subtypes (β2 and β3) is established by testing the ability of Vilanterol to elicit concentration-dependent increases in cAMP in CHO cells expressing human β1-, β2-, and β3-AR. Vilanterol is demonstrated to be highly selective for the β2-AR with at least a 1000-fold selectivity over both β2- and β3-AR subtypes. This analysis results in a low-affinity pKD for [3H]Vilanterol of 9.44±0.07 (n=4) in the presence Gpp(NH)p and a high-affinity pKD of 10.82±0.12 (n=4) and a low-affinity pKD 9.47±0.17 (n=4) in the absence of Gpp(NH)p. In addition, a low-affinity pKD for [3H]Vilanterol of 9.52±0.24 (n=4) in the absence of Gpp(NH)p (37°C) is observed. Vilanterol trifenatate is a novel inhaled long-acting β2-agonist with inherent 24 h activity in vitro in development as a combination with the inhaled corticosteroid fluticasone furoate for both COPD and asthma. Vilanterol is a novel long-acting β2-agonist (LABA) with inherent 24-hour activity for once-daily clinical treatment of chronic obstructive pulmonary disease (COPD) and asthma in combination with the inhaled novel corticosteroid fluticasone furoate, also active for 24 hours.
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