| Size | Price | Stock | Qty |
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| 250mg |
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| 500mg |
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| 1g |
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| 2g |
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| Other Sizes |
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Zafirlukast (ICI 204219) is a potent and orally bioavailable antagonist of leukotriene receptor (LTR) used for the maintenance treatment of asthma, often used in conjunction with an inhaled steroid and/or long-acting bronchodilator. It comes in tablet form, and the recommended dosage is twice daily. Telukast (Singulair), another leukotriene receptor antagonist, is administered once daily. Zileuton (Zyflo) is taken four times a day and is also used to treat asthma by inhibiting 5-lipoxygenase. Zafirlukast reduces airway constriction, mucus accumulation in the lungs, and breathing passage inflammation by blocking the action of cysteinyl leukotrienes on CysLT1 receptors.
| Targets |
leukotriene receptor
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|---|---|
| ln Vitro |
Zafirlukast possesses an N-methylindole moiety with a 3-alkyl substituent on the indole ring, which makes it similar to 3-methylindole. Zafirlukast readily forms a GSH adduct with a molecular mass of 880 Da upon incubation with horseradish peroxidase (10% conversion in 60 min). CYP3A4 is inactivated in a concentration-, time-, and NADP(H)-dependent manner by zafirlukast. In one report, zafirlukast was shown to inhibit CYP3A enzyme activity in vitro (nonpreincubation inhibition) with a Ki of 2 μM; however, higher values have been published, and our KI for the inactivation process is 13.4 μM. The high plasma protein binding of zafirlukast (>99%) would reduce the concentration of free drug. A highly electrophilic α,β-unsaturated iminium species is produced by two consecutive one-electron oxidations of zafirlukast, which then spontaneously reacts with GSH to produce the observed adduct.[1]
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| ln Vivo |
Zafirlukast is a potent and selective antagonist of the cysteinyl leukotriene receptor that is primarily used in the prevention of bronchial asthma. When administered orally at a dose of 80 mg/kg, zafirlukast significantly lowers tissue levels of myeloperoxidase, reduced glutathione, and catalase while having no effect on these parameters when administered rectal route.[2]
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| Animal Protocol |
Mice: It uses A/J female mice that are 5–6 weeks old. The first of two intraperitoneal injections (i.p.) of vinyl carbamate (16 mg/kg each, spaced seven days apart) is given to the mice when they are seven to eight weeks old. In their diet, the mice are given leukotriene inhibitors two weeks following their second dosage of vinyl carbamate. The meal should contain the prescribed mg/kg concentrations of zafirlukast (270 or 540 mg/kg), zileuton (600 or 1200 mg/kg), and MK-886 (30 mg/kg). After being exposed to leukotriene inhibitors for the first six weeks, mice are weighed every week. They are weighed every two to four weeks until they are sacrificed after that. Before being embedded in paraffin for histology, the lungs are removed, fixed for one night in formalin, moved to 70% alcohol, and checked for tumors.
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| References |
| Molecular Formula |
C31H33N3O6S
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|---|---|
| Molecular Weight |
575.6752
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| Exact Mass |
575.21
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| Elemental Analysis |
C, 64.68; H, 5.78; N, 7.30; O, 16.67; S, 5.57
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| CAS # |
107753-78-6
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| Related CAS # |
Zafirlukast-d7; 1217174-18-9; Zafirlukast-13C,d3; Zafirlukast-13C,d6
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| Appearance |
Solid powder
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| SMILES |
CC1=CC=CC=C1S(=O)(=O)NC(=O)C2=CC(=C(C=C2)CC3=CN(C4=C3C=C(C=C4)NC(=O)OC5CCCC5)C)OC
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| InChi Key |
YEEZWCHGZNKEEK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C31H33N3O6S/c1-20-8-4-7-11-29(20)41(37,38)33-30(35)22-13-12-21(28(17-22)39-3)16-23-19-34(2)27-15-14-24(18-26(23)27)32-31(36)40-25-9-5-6-10-25/h4,7-8,11-15,17-19,25H,5-6,9-10,16H2,1-3H3,(H,32,36)(H,33,35)
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| Chemical Name |
cyclopentyl N-[3-[[2-methoxy-4-[(2-methylphenyl)sulfonylcarbamoyl]phenyl]methyl]-1-methylindol-5-yl]carbamate
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| Synonyms |
ICI-204219; ICI204219; ICI 204219; ICI-204,219; ICI 204,219; ICI204,219; Zafirlukast; brand names Accolate, Accoleit, and Vanticon.
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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 |
| 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) |
DMSO: ~100 mg/mL (~173.7 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.61 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 (3.61 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. View More
Solubility in Formulation 3: 5%DMSO + 40%PEG300 + 5%Tween 80 + 50%ddH2O: 5.0mg/ml (8.69mM) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7371 mL | 8.6854 mL | 17.3708 mL | |
| 5 mM | 0.3474 mL | 1.7371 mL | 3.4742 mL | |
| 10 mM | 0.1737 mL | 0.8685 mL | 1.7371 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 |
| NCT04339140 | Recruiting | Drug: Zafirlukast | Ovarian Cancer | Beth Israel Deaconess Medical Center |
June 24, 2020 | Phase 2 |
| NCT06069063 | Not yet recruiting | Drug: Zafirlukast | Allergy to Cats | Allergy & Asthma Medical Group & Research Center |
January 5, 2024 | Phase 2 |
| NCT01283061 | Completed | Drug: Zafirlukast | Healthy | Dr. Reddy's Laboratories Limited | December 2007 | Phase 1 |
| NCT02950480 | Terminated | Drug: zafirlukast Other: Standard of Care (no intervention) |
Breast Cancer | University of California, San Francisco |
March 13, 2017 | Phase 2 |
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