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Arformoterol Tartrate

产品编号 T22245 CAS 200815-49-2

别名: (R,R)-Formoterol tartrate, 酒石酸福莫特罗

Arformoterol Tartrate ((R,R)-Formoterol 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。

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Arformoterol Tartrate Chemical Structure

Arformoterol Tartrate, CAS 200815-49-2

规格	价格/CNY	货期
1 mg	￥ 196	现货
5 mg	￥ 453	现货
10 mg	￥ 659	现货
25 mg	￥ 1,090	现货
50 mg	￥ 1,630	现货
100 mg	￥ 2,420	现货
200 mg	￥ 3,580	现货
1 mL * 10 mM (in DMSO)	￥ 539	现货

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Arformoterol Tartrate ((R,R)-Formoterol tartrate) is the tartrate salt of arformoterol. Arformoterol is a long-acting beta-2 adrenergic agonist with bronchodilator activity[2].
靶点活性	β2-adrenoceptor:2.9 nM (Kd)
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].

别名	(R,R)-Formoterol tartrate, 酒石酸福莫特罗
分子量	494.49
分子式	C23H30N2O10
CAS No.	200815-49-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 55 mg/ml (111.23 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0223 mL	10.1114 mL	20.2229 mL	50.5571 mL
	5 mM	0.4045 mL	2.0223 mL	4.0446 mL	10.1114 mL
	10 mM	0.2022 mL	1.0111 mL	2.0223 mL	5.0557 mL
	20 mM	0.1011 mL	0.5056 mL	1.0111 mL	2.5279 mL
	50 mM	0.0404 mL	0.2022 mL	0.4045 mL	1.0111 mL
	100 mM	0.0202 mL	0.1011 mL	0.2022 mL	0.5056 mL

计算器

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参考文献

1. Pahwa R , Soni V , Sharma P C , et al. Arformoterol Tartrate: A Review of Pharmacology, Analysis and Clinical Studies[J]. Tropical Journal of Pharmaceutical Research, 2011, 9(6). 2. Song W, et al. Postexposure administration of a {beta}2-agonist decreases chlorine-induced airway hyperreactivity in mice. Am J Respir Cell Mol Biol. 2011 Jul;45(1):88-94.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

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计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Arformoterol Tartrate 200815-49-2 GPCR/G Protein Neuroscience Adrenergic Receptor (R,R)-Formoterol tartrate Inhibitor (R,R)-Formoterol chronic Formoterol Tartrate obstructive 酒石酸福莫特罗 pulmonary Arformoterol COPD Beta Receptor inhibit inhibitor

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Arformoterol Tartrate

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

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剂量换算

体内实验配液计算器

技术支持

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