Salmeterol Xinafoate (GR 33343X xinafoate)

Alias: AHR 3929; AHR-3929; AH-3923; AH3923; Salmeterol xinafoate; GR-33343G; AHR3929; AH 3923; GR-33343X xinafoate; GR 33343X xinafoate; Salmetedur, Serevent®
Cat No.:V1101 Purity: ≥98%
Salmeterol Xinafoate (GR-33343G,AHR-3929; AH-3923; Salmetedur, Serevent), theXinafoate salt of Salmeterol,is a potent and long-acting β2-adrenergic receptor agonist with anti-inflammatory effects.
Salmeterol Xinafoate (GR 33343X xinafoate) Chemical Structure CAS No.: 94749-08-3
Product category: Adrenergic Receptor
This product is for research use only, not for human use. We do not sell to patients.
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Other Forms of Salmeterol Xinafoate (GR 33343X xinafoate):

  • Salmeterol
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

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.

Biological Activity I Assay Protocols (From Reference)
Targets
β2 adrenoceptor ( pEC50 = 9.6 ); β1 adrenoceptor ( pEC50 = 6.1 ); β3 adrenoceptor ( pEC50 = 5.9 )
ln Vitro

In vitro activity: Salmeterol (0.001-25 µM) suppresses the proliferation of human T cells[2].

ln Vivo
Salmeterol (0.16 mg/kg), formoterol (0.32 mg/kg), and their combination therapy have therapeutic effects in mice with chronic obstructive pulmonary disease (COPD)[3].
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.
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.
Animal Protocol
Male C57BL/6 mice (6-8 weeks old, body weight: 32-35 g)
Salmeterol (0.16 mg/kg) and/or Formoterol (0.32 mg/kg)
The therapeutic efficacy of co-treatment was investigated in this model over a 56-day-long observation period.
References

[1]. PThe discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating a urea group. Bioorg Med Chem. 2011 Oct 15;19(20):6026-32.

[2]. Effects of beta2-agonists on resident and infiltrating inflammatory cells. J Allergy Clin Immunol. 2002 Dec;110(6 Suppl):S282-90.

[3]. Efficacy of salmeterol and formoterol combination treatment in mice with chronic obstructive pulmonary disease. Exp Ther Med. 2018 Feb;15(2):1538-1545.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C36H45NO7
Molecular Weight
603.75
Exact Mass
603.32
Elemental Analysis
C, 71.62; H, 7.51; N, 2.32; O, 18.55
CAS #
94749-08-3
Appearance
Solid powder
SMILES
C1=CC=C(C=C1)CCCCOCCCCCCNCC(C2=CC(=C(C=C2)O)CO)O.C1=CC=C2C(=C1)C=CC(=C2O)C(=O)O
InChi Key
XTZNCVSCVHTPAI-UHFFFAOYSA-N
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)
Chemical Name
2-(hydroxymethyl)-4-[1-hydroxy-2-[6-(4-phenylbutoxy)hexylamino]ethyl]phenol;1-hydroxynaphthalene-2-carboxylic acid
Synonyms
AHR 3929; AHR-3929; AH-3923; AH3923; Salmeterol xinafoate; GR-33343G; AHR3929; AH 3923; GR-33343X xinafoate; GR 33343X xinafoate; Salmetedur, Serevent®
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~100 mg/mL (~165.6 mM)
Water: <1 mg/mL
Ethanol: ~4 mg/mL (~6.6 mM)
Solubility (In Vivo)
5%DMSO + Corn oil: 5.0mg/ml (8.28mM) (Please use freshly prepared in vivo formulations for optimal results.)
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.

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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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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.
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Clinical Trial Information
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
Biological Data
  • Salmeterol Xinafoate
    Salmeterol attenuates the inflammation of asthma induced by OVA and LPS.Cell Mol Immunol.2012May;9(3):267-75.
  • Salmeterol Xinafoate
    Salmeterol decreases the mRNA and protein levels of pro-inflammatory cytokines in LPS-activated DCs.Cell Mol Immunol.2012May;9(3):267-75.
  • Salmeterol Xinafoate
    Salmeterol inhibits MAPK and NF-κB activation.Cell Mol Immunol.2012May;9(3):267-75.
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