Salmeterol-xinafoate-GR-33343X-xinafoate-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESalmeterol xinafoateCat. No.: HY-17453CAS No.: 94749-08-3Synonyms: GR 33343X xinafoate分式: CHNO分量: 603.75作靶點(diǎn): Adrenergic Receptor作通路: GPCR/G Protein; Neuronal Signaling儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20

2、C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 50 mg/mL (82.82 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 1.6563 mL 8.2816 mL 16.5631 mL5 mM 0.3313 mL 1.6563 mL 3.3126 mL10 mM 0.1656 mL 0.8282 mL 1.6563 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活

3、性 Salmeterol xinafoate長效 2 腎上腺素能受體 (2AR) 激動劑，對WT 2AR的Ki值為 1.5 nM。IC50 & Target Ki: 1.5 nM (WT 2AR) 2體外研究Salmeterol significantly inhibits production of pro-inflammatory mediators by RAW264.7 and THP-1 cells.1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemESalmeterol downregulates PgLPS-mediated phos

4、phorylation of the ERK1/2 and JNK but not p38 MAPkinases (MAP-K). Salmeterol also attenuates the activation of NF-B via inhibition of nuclear translocation ofp65-NFB, the transcriptional activity of NF-B and IB phosphorylation 1. Salmeterol shows very highselectivity for the WT 2AR (1 Ki /2 Ki ratio

5、 of approximately 1500) with Ki of 1.50.4 nM 2. Salmeterolprevents phosphorylation levels of IRS-1Ser307 induced by tumor necrosis factor-. Salmeterol aloneprevents cell death in retinal Mller cells (p 3. Salmeterol (100 M) causes apoptosis of DCs, and can notaffect the differentiation and maturatio

6、n of DCs at 10 M. Salmeterol (10 M) decreases the mRNA andprotein levels of pro-inflammatory cytokines in LPS-activated DCs and inhibits MAPK and NF-B activation4.體內(nèi)研究 The OVA/LPS groups with salmeterol result in a significant decrease in the enhanced AHR in allergic mice ina dose-dependent manner.

7、Salmeterol contends with asthma via regulating the inflammation of the airway ofthe mice 4.PROTOCOLKinase Assay 2 The cells are rinsed twice with ice-cold phosphate-buffered saline and mechanically detached in ice-coldbuffer containing 10 mM TrisHCl, pH 7.4, 5 mM EDTA, 10 g/mL benzamidine, 10 g/mL s

8、oybean trypsininhibitor (type II-S), and 5 g/mL leupeptin (lysis buffer). The lysate is centrifuged at 45,000 g for 10 min at4C. The pellet is rehomogenized in lysis buffer, with a Potter-type homogenizer, and stored at 80C untiluse. The competition binding assays are performed in buffer containing

9、75 mM TrisHCl, pH 7.4, 12.5 mMMgCl2, and 2 mM EDTA, using 1-5 g of membrane protein, 50 pM 125I-CYP, and 0-100 M unlabeledligand in the presence of 100 M GTP, for 60 min at 37C. The binding reaction is terminated by dilution andrapid filtration through Whatman GF/C filters; the filters are washed th

10、ree times with solution containing 25mM TrisHCl, pH 7.4, and 1 mM MgCl2. Nonspecific binding is determined in the presence of 5 M ()-propranolol. The radioactivity on the filters is counted with a -counter.MCE has not independently confirmed the accuracy of these methods. They are for reference only

11、.Animal All mice are sensitized on days 0 and 14 by intraperitoneal injection of either PBS or 0.08 mg OVA and 0.1Administration 4 mL aluminum hydroxide in 0.1 mL of PBS (pH 7.4). After sensitization, animals are exposed to aerosolizedPBS-only (negative control), 1% OVS/PBS (acute exposure), 1% OVA/

12、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 (days24-26). On day 27, the mice are killed and lungs are divided into two groups for analysis: the left lung lobesare lavaged three times with 1 mL of PBS with 1% fet

13、al calf serum and 5 U/mL heparin, and the right halvesare fixed by 4% paraformaldehyde for histological analysis.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Sharma M, et al. Salmeterol; A Long Acting 2-Aderenergic Receptor Agonist Inhib

14、its Macrophage Activation by LipopolysaccharideFrom 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. MolPharmacol. 1998 Oct;54(4):616-22.2/3 Master of Small Molec

15、ules 您邊的抑制劑師www.MedChemE3. Walker RJ, Anderson NM, Bahouth S, Silencing of insulin receptor substrate-1 increases cell death in retinal Mller 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 ofdendritic cells. Cell Mol Imm