Zafirlukast
Based on 4 publication(s) in Google Scholar
Zafirlukast (ICI 204219) is a potent orally active leukotriene D4 (LTD4) receptor antagonist. Zafirlukast shows anti-asthmatic, anti-inflammatory and anti-bacterial effects.
For research use only. We do not sell to patients.
- Purity: 99.87%
- CAS No.: 107753-78-6
- Formula: C31H33N3O6S
- Molecular Weight:575.68
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Zafirlukast
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Bio/Physico-chemical Assay
All Leukotriene Receptor Isoforms
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Biological Activity
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LTD4 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
18.1 μM
Compound: 34
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Inhibition of microsomal PGES1 in ILbeta/TNFalpha-stimulated human A549 cells using PGH2 as substrate preincubated for 15 mins followed by substrate addition measured after 1 min by LC-MS/MS analysis
Inhibition of microsomal PGES1 in ILbeta/TNFalpha-stimulated human A549 cells using PGH2 as substrate preincubated for 15 mins followed by substrate addition measured after 1 min by LC-MS/MS analysis
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10.1039/C5MD00278H |
| HEK293 | IC50 |
0.014 μM
Compound: Accolate
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Antagonist activity against CysLT1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
Antagonist activity against CysLT1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
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[PMID: 26985325] |
| HEK293 | IC50 |
1.3 μM
Compound: zafirlukast
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Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
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[PMID: 23241029] |
| HEK293 | IC50 |
58 μM
Compound: Accolate
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Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
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[PMID: 26985325] |
| HEK293 | IC50 |
7.6 μM
Compound: zafirlukast
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Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
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[PMID: 23241029] |
| HEK293 | IC50 |
9.7 μM
Compound: zafirlukast
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Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay
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[PMID: 23241029] |
| HEK-293T | IC50 |
7397 nM
Compound: zafirlukast
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Antagonist activity at human CysLT2 expressed in HEK293T cells assessed as inhibition of LTC4-induced effect preincubated for 30 mins prior to LTC4 addition by Aequorin luminescence assay
Antagonist activity at human CysLT2 expressed in HEK293T cells assessed as inhibition of LTC4-induced effect preincubated for 30 mins prior to LTC4 addition by Aequorin luminescence assay
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[PMID: 26200813] |
| HepG2 | EC50 |
14.1 μM
Compound: Zafirlukast
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Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis
Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis
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[PMID: 20966043] |
| HepG2 | EC50 |
58.4 μM
Compound: Zafirlukast
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Activation of rat PXR expressed in human HepG2 cells after 24 hrs by luciferase reporter gene based luminescent analysis
Activation of rat PXR expressed in human HepG2 cells after 24 hrs by luciferase reporter gene based luminescent analysis
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[PMID: 20966043] |
| HepG2 | EC50 |
9.5 μM
Compound: Zafirlukast
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Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis
Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis
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[PMID: 20966043] |
| HGC-27 | IC50 |
44 μM
Compound: 1; ZAF
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Cytotoxicity against human HGC-27 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay
Cytotoxicity against human HGC-27 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay
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[PMID: 36622814] |
| U2OS | IC50 |
6.5 μM
Compound: Zafirlukast
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Inhibition of HA-tagged human NTCP expressed in human U2OS cells assessed as reduction in [14C]taurocholate uptake preincubated for 10 mins followed by [14C] taurocholate addition and further incubation for 10 mins by scintillation counting method
Inhibition of HA-tagged human NTCP expressed in human U2OS cells assessed as reduction in [14C]taurocholate uptake preincubated for 10 mins followed by [14C] taurocholate addition and further incubation for 10 mins by scintillation counting method
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[PMID: 31439379] |
| U-937 | IC50 |
0.001 μM
Compound: 1
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Compound was evaluated for influx of calcium mobilization in human U937 cells
Compound was evaluated for influx of calcium mobilization in human U937 cells
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[PMID: 9873435] |
| U-937 | IC50 |
0.001 μM
Compound: 1
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Compound was tested for its ability to inhibit calcium influx in human U937 cells
Compound was tested for its ability to inhibit calcium influx in human U937 cells
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[PMID: 9934474] |
| U-937 | IC50 |
1 nM
Compound: 1
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Ability to mobilize Ca+2 in LTD4 dependent Ca+2 mobilization assay in differentiated human monocytic U-937 cells
Ability to mobilize Ca+2 in LTD4 dependent Ca+2 mobilization assay in differentiated human monocytic U-937 cells
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[PMID: 9873560] |
| U-937 | IC50 |
1 nM
Compound: Zafirlukast
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In vitro blocking of extracellular calcium mobilization in human U937 cells
In vitro blocking of extracellular calcium mobilization in human U937 cells
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[PMID: 10509933] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 107753-78-6
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Appearance Solid
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Molecular Weight 575.68
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Formula C31H33N3O6S
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Color Off-white to pink
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SMILES
O=C(OC1CCCC1)NC2=CC3=C(N(C)C=C3CC4=CC=C(C(NS(=O)(C5=CC=CC=C5C)=O)=O)C=C4OC)C=C2
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Synonyms
ICI 204219
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (4)
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Journal Impact Factor
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Most Recent
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Proc Natl Acad Sci U S A
Peptide-based allosteric inhibitor targets TNFR1 conformationally active region and disables receptor-ligand signaling complex. [Abstract]2024 Apr 2;121(14):e2308132121. PMID: 38551841
Zafirlukast purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2024 Apr 2;121(14):e2308132121. [Abstract]
Zafirlukast (ZAF) (100 µM) disrupted TNFR1 ECD–ECD interaction or receptor dimerization.
Zafirlukast purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2024 Apr 2;121(14):e2308132121. [Abstract]
Zafirlukast (ZAF) (100 µM) reduced FRET in the PLAD biosensor.
Zafirlukast purchased from MedChemExpress. Usage Cited in: Proc Natl Acad Sci U S A. 2024 Apr 2;121(14):e2308132121. [Abstract]
Treatment of Zafirlukast (ZAF) (100 µM) to the TNFR1 FRET biosensor to test whether FKC affects the FRET reduction induced by Zafirlukast (ZAF).
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ACS Appl Mater Interfaces
Targeting Tumor Necrosis Factor Receptor 1 with Selected Aptamers for Anti-Inflammatory Activity. [Abstract]2023 Mar 8;15(9):11599-11608. PMID: 36812453
Zafirlukast purchased from MedChemExpress. Usage Cited in: ACS Appl Mater Interfaces. 2023 Mar 8;15(9):11599-11608. [Abstract]
Western blotting and quantification of inhibitory effect of Zafirlukast (Zaf) (200 μM) on the TNFα-mediated NF-κB pathway in L929 cells.
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J Mol Histol
Zafirlukast promotes mitochondrial respiration by stimulating mitochondrial biogenesis in human bronchial epithelial cells. [Abstract]2021 Aug;52(4):643-650. PMID: 33977464
Zafirlukast purchased from MedChemExpress. Usage Cited in: J Mol Histol. 2021 Aug;52(4):643-650. [Abstract]
Zafirlukast (5 μM; 48 h) greatly increased the oxygen consumption rate (OCR) in human bronchial epithelial cells.
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Solvent & Solubility
DMSO : 100 mg/mL (173.71 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.61 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Mice[2]
Female A/J mice (5-6 weeks of age) are used. When the mice are 7-8 weeks of age, they are administered the first of two i.p. injections of vinyl carbamate of 16 mg/kg each and 7 days apart. Two weeks after the second dose of vinyl carbamate, the mice receive the leukotriene inhibitors in their diet. Zafirlukast (270 or 540 mg/kg), Zileuton (600 or 1200 mg/kg), and MK-886 (30 mg/kg) is provided at the indicated mg/kg concentrations in the diet. Mice are weighed weekly through the first 6 weeks of exposure to the leukotriene inhibitors. After which, they are then weighed every 2-4 weeks until sacrificed. Mice are sacrificed by carbon dioxide asphyxiation after 13 and 43 weeks of exposure to the drugs. The lungs are harvested, fixed overnight in formalin, transferred to 70% alcohol, and evaluated for tumors before embedding in paraffin for histology[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (275 KB)
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SDS (597 KB)
- English - EN (597 KB)
- Français - FR (597 KB)
- Deutsch - DE (597 KB)
- Norwegian - NO (597 KB)
- Español - ES (597 KB)
- Swedish - SV (597 KB)
- Italian - IT (597 KB)
- Portuguese - PT (597 KB)
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Handling Instructions (2659 KB)
References
[1]. Finnerty JP, et al. Role of leukotrienes in exercise-induced asthma. Inhibitory effect of ICI 204219, a potent leukotriene D4 receptor antagonist. Am Rev Respir Dis. 1992 Apr;145(4 Pt 1):746-9. [Content Brief]
[2]. Gunning WT, et al. Chemoprevention by lipoxygenase and leukotriene pathway inhibitors of vinyl carbamate-induced lung tumors in mice. Cancer Res. 2002 Aug 1;62(15):4199-201. [Content Brief]
[3]. Lei C, et al. Zafirlukast attenuates advanced glycation end-products (AGEs)-induced degradation of articular extracellular matrix (ECM). Int Immunopharmacol. 2019;68:68-73. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7371 mL | 8.6854 mL | 17.3708 mL | 43.4269 mL |
| 5 mM | 0.3474 mL | 1.7371 mL | 3.4742 mL | 8.6854 mL | |
| 10 mM | 0.1737 mL | 0.8685 mL | 1.7371 mL | 4.3427 mL | |
| 15 mM | 0.1158 mL | 0.5790 mL | 1.1581 mL | 2.8951 mL | |
| 20 mM | 0.0869 mL | 0.4343 mL | 0.8685 mL | 2.1713 mL | |
| 25 mM | 0.0695 mL | 0.3474 mL | 0.6948 mL | 1.7371 mL | |
| 30 mM | 0.0579 mL | 0.2895 mL | 0.5790 mL | 1.4476 mL | |
| 40 mM | 0.0434 mL | 0.2171 mL | 0.4343 mL | 1.0857 mL | |
| 50 mM | 0.0347 mL | 0.1737 mL | 0.3474 mL | 0.8685 mL | |
| 60 mM | 0.0290 mL | 0.1448 mL | 0.2895 mL | 0.7238 mL | |
| 80 mM | 0.0217 mL | 0.1086 mL | 0.2171 mL | 0.5428 mL | |
| 100 mM | 0.0174 mL | 0.0869 mL | 0.1737 mL | 0.4343 mL |
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