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Salmeterol Xinafoate

产品编号 T6653 CAS 94749-08-3

别名: Salmetedur, 昔美酸沙美特罗, 沙美特罗昔萘酸酯, GR 33343X xinafoate, Arial

Salmeterol Xinafoate (GR 33343X xinafoate) 是选择性人β2肾上腺素受体激动剂。Salmeterol 有效刺激 cAMP 积累，能够作用于 CHO 细胞，对人β2，β1和β3肾上腺素受体的 pEC50分别为 9.6、6.1 和 5.9。

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Salmeterol Xinafoate, CAS 94749-08-3

规格	价格/CNY	货期
1 mg	￥ 183	现货
5 mg	￥ 397	现货
10 mg	￥ 672	现货
25 mg	￥ 1,330	现货
50 mg	￥ 2,170	现货
100 mg	￥ 3,670	待询
1 mL * 10 mM (in DMSO)	￥ 543	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	Salmeterol Xinafoate (GR 33343X xinafoate) is a long-acting β2-adrenergic receptor agonist with anti-inflammatory effects, used in the treatment of asthma symptoms and chronic obstructive pulmonary disease (COPD) symptoms.
靶点活性	β2-adrenoceptor (WT):Ki:1.5 nM
体外活性	Salmeterol significantly inhibits production of pro-inflammatory mediators by RAW264.7 and THP-1 cells. Salmeterol downregulates PgLPS-mediated phosphorylation of the ERK1/2 and JNK but not p38 MAP kinases (MAP-K). Salmeterol also attenuates the activation of NF-κB via inhibition of nuclear translocation of p65-NFκB, the transcriptional activity of NF-κB and IκBα phosphorylation. Salmeterol shows very high selectivity for the WT β2AR (β1 Ki /β2 Ki ratio of approximately 1500) with Ki of 1.5±0.4 nM. Salmeterol prevents phosphorylation levels of IRS-1Ser307 induced by tumor necrosis factor-α. Salmeterol alone prevents cell death in retinal Müller cells (p<0.05 versus 25 mM glucose). Salmeterol in conbination with IRS-1 shRNA shows a significant increase in cell death compared to salmeterol alone. Moreover, salmeterol alone treatment significantly reduces cytochrome C levels, with the effect lessened when salmeterol is combined with IRS-1 shRNA. Salmeterol (100 μM) causes apoptosis of DCs, and can not affect the differentiation and maturation of DCs at 10 μM. Salmeterol (10 μM) decreases the mRNA and protein levels of pro-inflammatory cytokines in LPS-activated DCs and inhibits MAPK and NF-κB activation
体内活性	The OVA/LPS groups with salmeterol result in a significant decrease in the enhanced AHR in allergic mice in a dose-dependent manner. Salmeterol contends with asthma via regulating the inflammation of the airway of the mice.
激酶实验	The cells are rinsed twice with ice-cold phosphate-buffered saline and mechanically detached in ice-cold buffer containing 10 mM Tris·HCl, pH 7.4, 5 mM EDTA, 10 μg/mL benzamidine, 10 μg/mL soybean trypsin inhibitor (type II-S), and 5 μg/mL leupeptin (lysis buffer). The lysate is centrifuged at 45,000 ×g for 10 min at 4°C. The pellet is rehomogenized in lysis buffer, with a Potter-type homogenizer, and stored at ?80°C until use. The competition binding assays are performed in buffer containing 75 mM Tris·HCl, pH 7.4, 12.5 mM MgCl2, and 2 mM EDTA, using 1-5 μg of membrane protein, 50 pM 125I-CYP, and 0-100 μM unlabeled ligand in the presence of 100 μM GTP, for 60 min at 37°C. The binding reaction is terminated by dilution and rapid filtration through Whatman GF/C filters; the filters are washed three times with solution containing 25 mM Tris·HCl, pH 7.4, and 1 mM MgCl2. Nonspecific binding is determined in the presence of 5 μM (±)-propranolol. The radioactivity on the filters is counted with a γ-counte
动物实验	Salmeterol is formulated in PBS.All mice are sensitized on days 0 and 14 by intraperitoneal injection of either PBS or 0.08 mg OVA and 0.1 mL aluminum hydroxide in 0.1 mL of PBS (pH 7.4). After sensitization, animals are exposed to aerosolized PBS-only (negative control), 1% OVS/PBS (acute exposure), 1% OVA/0.01% LPS/PBS (extra LPS exposure) or 1% OVA/0.01% LPS/salmeterol/PBS (sal treatment) for 40 min, once per day for 3 consecutive days (days 24-26). On day 27, the mice are killed and lungs are divided into two groups for analysis: the left lung lobes are lavaged three times with 1 mL of PBS with 1% fetal calf serum and 5 U/mL heparin, and the right halves are fixed by 4% paraformaldehyde for histological analysis.

别名	Salmetedur, 昔美酸沙美特罗, 沙美特罗昔萘酸酯, GR 33343X xinafoate, Arial
分子量	603.75
分子式	C36H45NO7
CAS No.	94749-08-3

存储

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

溶解度

Ethanol: 12.1 mg/mL (20 mM)

DMSO: 60.4 mg/mL (100 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
Ethanol / DMSO	1 mM	1.6563 mL	8.2816 mL	16.5631 mL	41.4079 mL
	5 mM	0.3313 mL	1.6563 mL	3.3126 mL	8.2816 mL
	10 mM	0.1656 mL	0.8282 mL	1.6563 mL	4.1408 mL
	20 mM	0.0828 mL	0.4141 mL	0.8282 mL	2.0704 mL
DMSO	50 mM	0.0331 mL	0.1656 mL	0.3313 mL	0.8282 mL
DMSO	100 mM	0.0166 mL	0.0828 mL	0.1656 mL	0.4141 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Isogaya M, et al. Identification of a key amino acid of the beta2-adrenergic receptor for high affinity binding of salmeterol. Mol Pharmacol. 1998 Oct;54(4):616-22. 2. Walker, R., Anderson, N., BAhouth, S., & Steinle, J. (2012). Silencing of insulin receptor substrate-1 increases cell death in retinal Müller cells. Mol Vis, 18(27), 271-9. 3. Hu Z, et al. Salmeterol attenuates the inflammatory response in asthma and decreases the pro-inflammatory cytokine secretion of dendritic cells. Cell Mol Immunol. 2012 May;9(3):267-75.

文献引用

1. Zhao J, Xu L, Bai Y, et al.The efficacy and mechanism of salmeterol against influenza A virus in vitro and in vivo.International Immunopharmacology.2023, 119: 110226.

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+

% +

% Tween 80+

% ddH₂O

%DMSO+

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

Salmeterol Xinafoate 94749-08-3 GPCR/G Protein Microbiology/Virology Neuroscience Proteases/Proteasome HIV Protease Adrenergic Receptor corticosteroid Salmetedur 昔美酸沙美特罗 Salmeterol 沙美特罗昔萘酸酯 Beta Receptor therapy inhibit GR 33343X xinafoate GR 33343X Arial combination agonist inflammatory Inhibitor inhibitor

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Salmeterol Xinafoate

存储

溶解度

溶液配制表

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输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

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剂量换算

体内实验配液计算器

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