{{cart_num}}
My CartCAS：94749-08-3
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
Qty：
Size：
| CAS | 94749-08-3 |
| Name | Salmeterol Xinafoate |
| Molecular Formula | C25H37NO4·C11H8O3 |
| Molecular Weight | 603.75 |
| Solubility | Soluble in DMSO ≥5mg/mL |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD00897708 |
| SMILES | O=C(C1=CC=C2C=CC=CC2=C1O)O.OC3=C(CO)C=C(C(CNCCCCCCOCCCCC4=CC=CC=C4)O)C=C3 |
| InChIKey | XTZNCVSCVHTPAI-UHFFFAOYSA-N |
| InChI | InChI=1S/C25H37NO4.C11H8O3/c27-20-23-18-22(13-14-24(23)28)25(29)19-26-15-7-1-2-8-16-30-17-9-6-12-21-10-4-3-5-11-21;12-10-8-4-2-1-3-7(8)5-6-9(10)11(13)14/h3-5,10-11,13-14,18,25-29H,1-2,6-9,12,15-17,19-20H2;1-6,12H,(H,13,14) |
| PubChem CID | 56801 |
| Target Point | Adrenergic Receptor |
| Passage | Endocrinology & Hormones;GPCR & G Protein;Neuronal Signaling |
| Background | Salmeterol Xinafoate is a long-acting β2-adrenergic receptor agonist. |
| Biological Activity | Salmeterol xinafoate 是长效 β2 肾上腺素能受体 (β2AR) 激动剂，对WT β2AR的Ki值为 1.5 nM。[1-4] |
| IC50 | Ki: 1.5nM(WT β2AR)[2] |
| In Vitro | 沙美特罗显著抑制RAW264.7和THP-1细胞产生促炎介质。沙美特罗下调PgLPS介导的ERK1 / 2和JNK的磷酸化，但不下调p38 MAP激酶(MAP-K)。沙美特罗还通过抑制p65-NFκB的核转位，NF-κB的转录活性和IκBα磷酸化来减弱NF-κB的活化[1]。沙美特罗对WTβ2AR的选择性非常高(β1Ki /β2Ki比值约为1500)，Ki为1.5±0.4 nM [2]。沙美特罗可防止肿瘤坏死因子-α诱导的IRS-1Ser307的磷酸化水平。沙美特罗单独防止视网膜Müller细胞中的细胞死亡(p <0.05对25mM葡萄糖)。与单独的沙美特罗相比，与IRS-1shRNA组合的沙美特罗显示细胞死亡显著增加。此外，单用沙美特罗治疗可显著降低细胞色素C水平，当沙美特罗与IRS-1 shRNA结合时，效果会降低[3]。沙美特罗(100μM)引起DC的凋亡，并且不会影响10μM的DC的分化和成熟。沙美特罗(10μM)降低LPS激活的DC中促炎细胞因子的mRNA和蛋白水平，并抑制MAPK和NF-κB活化[4]。 |
| In Vivo | 含有沙美特罗的OVA / LPS组以剂量依赖性方式导致过敏小鼠中增强的AHR显著降低。沙美特罗通过调节小鼠气道的炎症来对抗哮喘[4]。 |
| Animal Experiment | 通过腹膜内注射PBS或0.08mg OVA和0.1mL氢氧化铝的0.1mL PBS(pH7.4)，在第0天和第14天使所有小鼠致敏。致敏后，将动物暴露于仅雾化的PBS(阴性对照)，1％OVS / PBS(急性暴露)，1％OVA / 0.01％LPS / PBS(额外LPS暴露)或1％OVA / 0.01％LPS /沙美特罗/ PBS(sal处理)40分钟，每天一次，连续3天(第24-26天)。在第27天，将小鼠杀死并将肺分成两组进行分析：用1mL含1％胎牛血清和5U / mL肝素的PBS灌洗左肺叶三次，并将右半部分固定用4％多聚甲醛进行组织学分析。 |
| Kinase Experiment | 用冰冷的磷酸盐缓冲盐水冲洗细胞两次，并在含有10mM Tris·HCl，pH 7.4，5mM EDTA，10μg/ mL苯甲脒，10μg/ mL大豆胰蛋白酶抑制剂(类型)的冰冷缓冲液中机械分离。 II-S)和5μg/ mL亮肽素(裂解缓冲液)。将裂解物在4℃以45，000×g离心10分钟。用Potter型均化器将沉淀在裂解缓冲液中再均化，并在-80℃下储存直至使用。竞争结合测定在含有75mM Tris·HCl，pH 7.4，12.5mM MgCl 2和2mM EDTA的缓冲液中进行，使用1-5μg膜蛋白，50μM125I-CYP和0-100μM未标记配体。在37°C下存在100μMGTP60分钟。通过Whatman GF / C过滤器稀释和快速过滤终止结合反应;用含有25mM Tris·HCl，pH7.4和1mM MgCl2的溶液洗涤滤膜三次。在5μM(±)- 普萘洛尔存在下测定非特异性结合。用γ计数器计算滤器上的放射性。 |
| Data Literature Source | [1]. Sharma M，et al. Salmeterol; A Long Acting β2-Aderenergic Receptor Agonist Inhibits Macrophage Activation by Lipopolysaccharide From Porphyromonas Gingivalis. J Periodontol. 2017 Mar 3:1-17. [2]. 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. [3]. Walker RJ，Anderson NM，Bahouth S，Silencing of insulin receptor substrate-1 increases cell death in retinal Müller cells. Mol Vis. 2012;18:271-9. Epub 2012 Feb 1. [4]. 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. |
| Unit | Bottle |
| Specification | 5mg 10mg |
是一种长效的β2-adrenergic receptor激动剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
Note：
1. The products are all for scientific research use only. Do not use it for medical, clinical diagnosis or treatment, food and cosmetics, etc. Do not store them in ordinary residential areas.
2. For your safety and health, please wear laboratory clothes, disposable gloves and masks.
3. The experimental results may be affected by many factors, after-sale service is limited to the product itself and does not involve other compensation.
Sorry, there is no more information.
Manual Download
