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Purity: ≥98%
Salmeterol Xinafoate (GR-33343G, AHR-3929; AH-3923; Salmetedur, Serevent), the Xinafoate salt of Salmeterol, is a potent and long-acting β2-adrenergic receptor agonist with anti-inflammatory effects. It binds to the WT β2-adrenergic receptor and activates it at a Ki of 1.5 nM. Salmeterol is primarily used to treat chronic obstructive pulmonary disease, or COPD, and asthma. Breathlessness, wheezing, coughing, and tightness in the chest are some of these symptoms. Salmeterol is also used to avoid exercise-induced bronchospasm, a condition that causes breathing difficulties.
| Targets |
β2 adrenoceptor ( pEC50 = 9.6 ); β1 adrenoceptor ( pEC50 = 6.1 ); β3 adrenoceptor ( pEC50 = 5.9 )
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| Enzyme Assay |
After twice being rinsed with ice-cold phosphate-buffered saline, the cells are mechanically detached in an ice-cold buffer that contains 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). 10 minutes at 4°C are spent centrifuging the lysate at 45,000 ×g. Using a Potter-xstyle homogenizer, the pellet is rehomogenized in lysis buffer and kept at -80°C until needed. The competition binding assays are run for 60 minutes at 37°C with 1–5 μg of membrane protein, 50 pM 125I–CYP, and 0-100 μM unlabeled ligand in the presence of 100 μM GTP in a buffer containing 75 mM Tris·HCl, pH 7.4, 12.5 mM MgCl2, and 2 mM EDTA. Whatman GF/C filters are quickly diluted and rapidly filtered through them to stop the binding reaction. The filters are then three times washed with a solution containing 25 mM Tris·HCl, pH 7.4, and 1 mM MgCl2. Nonspecific binding is assessed when 5 μM (±)-propranolol is present. Using a γ-counter, the radioactivity on the filters is measured.
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| Cell Assay |
Salmeterol dramatically reduces RAW264.7 and THP-1 cells' ability to produce pro-inflammatory mediators. Salmeterol inhibits phosphorylation of ERK1/2 and JNK by PgLPS, but not p38 MAP kinases (MAP-K). Moreover, salmeterol inhibits p65-NFκB's nuclear translocation, NF-κB transcriptional activity, and IκBα phosphorylation to lessen NF-κB activation. Salmeterol exhibits extremely high selectivity with a Ki of 1.5±0.4 nM for the WT β2AR (β1 Ki /β2 Ki ratio of roughly 1500). Salmeterol inhibits IRS-1Ser307 phosphorylation levels brought on by tumor necrosis factor-α. In retinal Müller cells, salmeterol alone inhibits cell death (p<0.05 compared to 25 mM glucose). When combined with IRS-1shRNA, salmeterol significantly increases cell death as compared to when used alone. Furthermore, treatment with salmeterol alone dramatically lowers cytochrome C levels; however, this effect is mitigated when salmeterol is coupled with IRS-1 shRNA. At 10 μM, salmeterol has no effect on the differentiation and maturation of DCs; instead, it induces apoptosis in DCs. Salmeterol (10 μM) inhibits the activation of MAPK and NF-κB and reduces the mRNA and protein levels of pro-inflammatory cytokines in LPS-activated DCs.
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| Animal Protocol |
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| References |
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| Additional Infomation |
Salmeterol xinafoate is a naphthoic acid.
A selective ADRENERGIC BETA-2 RECEPTOR agonist that functions as a BRONCHODILATOR when administered by inhalation. It is used to manage the symptoms of ASTHMA and CHRONIC OBSTRUCTIVE PULMONARY DISEASE. See also: Salmeterol (has active moiety); Fluticasone propionate; salmeterol xinafoate (component of). |
| Molecular Formula |
C36H45NO7
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| Molecular Weight |
603.75
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| Exact Mass |
603.319
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| Elemental Analysis |
C, 71.62; H, 7.51; N, 2.32; O, 18.55
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| CAS # |
94749-08-3
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| Related CAS # |
Salmeterol; 89365-50-4; Salmeterol-d3 xinafoate; Salmeterol-13C6 xinafoate
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| PubChem CID |
56801
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| Appearance |
White to off-white solid powder
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| Density |
1.112g/cm3
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| Boiling Point |
603ºC at 760 mmHg
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| Melting Point |
137-138ºC
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| Flash Point |
318.5ºC
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| Index of Refraction |
1.565
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| LogP |
6.741
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
17
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| Heavy Atom Count |
44
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| Complexity |
629
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C1C(O)=C2C(C=CC=C2)=CC=1)O.OC1C(CO)=CC(C(CNCCCCCCOCCCCC2C=CC=CC=2)O)=CC=1
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| InChi Key |
XTZNCVSCVHTPAI-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
2-(hydroxymethyl)-4-[1-hydroxy-2-[6-(4-phenylbutoxy)hexylamino]ethyl]phenol;1-hydroxynaphthalene-2-carboxylic acid
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.45 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.45 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.45 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 5%DMSO + Corn oil: 5.0mg/ml (8.28mM) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6563 mL | 8.2816 mL | 16.5631 mL | |
| 5 mM | 0.3313 mL | 1.6563 mL | 3.3126 mL | |
| 10 mM | 0.1656 mL | 0.8282 mL | 1.6563 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05982990 | Active Recruiting |
Drug: ADVAIR DISKUS® 250/50 Drug: Fluticasone propionate 250 mcg and salmeterol xinafoate 50 mcg/Respirent Pharmaceuticals |
Bioequivalence | Respirent Pharmaceuticals Co Ltd. | August 1, 2023 | Phase 1 |
| NCT05697003 | Active Recruiting |
Drug: ADVAIR DISKUS 100/50 Drug: Fluticasone propionate 1000 mcg and salmeterol xinafoate 50 mcg/Respirent Pharmaceuticals |
Bioequivalence | Respirent Pharmaceuticals Co Ltd. | February 17, 2023 | Phase 1 |
| NCT04503460 | Recruiting | Drug: Salmeterol Xinafoate Drug: Salmeterol Fluticasone |
Asthma | Imperial College London | July 23, 2021 | Phase 4 |
| NCT05776927 | Not yet recruiting | Drug: QVM149 Drug: Placebo to QVM149 Drug: Run-In Medication |
Asthma | Novartis Pharmaceuticals | December 23, 2024 | Phase 3 |
| NCT00576069 | NCT00576069 | Drug: budesonide/formoterol Drug: fluticasone/salmeterol |
Asthma | Gelb, Arthur F., M.D. | October 25, 2007 | N/A |
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