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Arformoterol Tartrate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Arformoterol Tartrate图片
CAS NO:200815-49-2
包装与价格:
包装价格(元)
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
500 mg电议

产品名称
(R,R)-Formoterol tartrate
酒石酸福莫特罗
产品介绍
Arformoterol Tartrate 是一种长效 β2-肾上腺素能受体 (β2-AR) 激动剂,Kd=2.9 nM。它是一种 Formoterol 的 (R,R)-对映异构体,可用于慢性阻塞性肺疾病 (COPD) 的研究。

产品描述

Arformoterol Tartrate is the tartrate salt of arformoterol. Arformoterol is a long-acting beta-2 adrenergic agonist with bronchodilator activity[2].

体内活性

Arformoterol (R,R-formoterol) is a active isomer of racemic formoterol and is indicated for the long-term, maintenance treatment of bronchoconstriction in patients with COPD including chronic bronchitis and emphysema. It is a potent and selective agent which causes bronchial smooth muscle relaxation and inhibits the release of inflammatory mediators. Its pharmacological effects can be attributed to the increased intracellular cyclic adenosine monophosphate (cAMP) levels that result from the stimulation of intracellular adenyl cyclase. Arformoterol tartrate is well absorbed through lungs when administered by a nebulizer. The mean peak plasma concentration (Cmax) and systemic exposure (AUC0-12h) are 4.3 pg/mL and 34.5 pg.h/mL, respectively, when 15 μg arformoterol is administered every 12 h for 14 days in COPD patients. The time to achieve median steady state peak plasma concentration (tmax) is approximately half an hour after drug administration. The mean terminal half-life is 26 h in COPD patients when treated with 15 μg inhaled arformoterol twice daily for 14 days. The binding of arformoterol to human plasma proteins in vitro is 52-65% at concentrations of 0.25, 0.5 and 1.0 ng/mL of radiolabeled arformoterol. Metabolism occurs primarily by direct conjugation (glucuronidation) and secondary route of metabolism is via O-demethylation. Metabolism is mediated by atleast five human uridine diphosphoglucuronosyltransferase (UGT) isozymes as well as CYP2D6 and CYP2C19. After administration of a single oral dose of radiolabeled arformoterol, 63% of the radioactive amount was recovered in urine and 11% in feces within 48 h. A total of 89% of the total radioactive dose was recovered within 14 days, with 67% in urine and 22% in faeces[1].

动物实验

Exposure of C57BL/6 mice(8 wk old) to 400 ppm Cl(2) for 30 minutes increased respiratory system resistance and airway responsiveness to aerosolized methacholine. Intranasal administration of arformoterol mitigated the Cl(2) effects on airway reactivity and AFC, presumably by increasing lung cyclic AMP level. Arformoterol did not modify the inflammatory responses, as evidenced by the number of inflammatory cells and concentrations of IL-6 and TNF-α in the bronchoalveolar lavage. NF-κB activity (assessed by p65 Western blots and electrophoretic mobility shift assay) remained at control levels up to 24 hours after Cl(2) exposure. Our results provide mechanistic insight into the effectiveness of long-term β(2)-agonists in reversing Cl(2)-induced reactive airway dysfunction syndrome and injury to distal lung epithelial cells[2].

Cas No.

200815-49-2

分子式

C23H30N2O10

分子量

494.497

别名

(R,R)-Formoterol tartrate;酒石酸福莫特罗

储存和溶解度

DMSO:55 mg/ml (111.23 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years