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Technical Data
| Formula | C31H33N3O6S |
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| Molecular Weight | 575.68 | CAS No. | 107753-78-6 | |
| Solubility (25°C)* | In vitro | DMSO | 115 mg/mL (199.76 mM) | |
| Water | Insoluble | |||
| Ethanol | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Biological Activity
| Description | Zafirlukast is an oral leukotriene receptor antagonist (LTRA), used to prevent asthma symptoms. | |
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| In vitro | Zafirlukast is similar to 3-methylindole because it contains an N-methylindole moiety that has a 3-alkyl substituent on the indole ring. Zafirlukast readily forms (10% conversion in 60 min) a GSH adduct with molecular mass of 880 Da upon incubation with horseradish peroxidase. Zafirlukast produces time-, concentration-, and NADP(H)-dependent inactivation of CYP3A4. Zafirlukast is shown to inhibit CYP3A enzyme activity in vitro (nonpreincubation inhibition) with a Ki of 2 μM in one report, but higher values have been published, and our KI for the inactivation process is 13.4 μM. Zafirlukast has high plasma protein binding (>99%), which would lower the free-drug concentration. Zafirlukast undergoes two successive one-electron oxidations to afford a highly electrophilic α,β-unsaturated iminium species, which reacts spontaneously with GSH to yield the observed adduct. [1] | |
| In vivo | Zafirlukast is a potent and selective cysteinyl leukotriene receptor antagonist which is used mainly in the prophylaxis of bronchial asthma. Zafirlukast in a dose of 80 mg/kg orally produces a significant decrease in tissue malondialdehyde, myeloperoxidase, and an increase in both reduced glutathione and catalase levels, while there is no significant changes with the rectal route. [2] |
Protocol (from reference)
References
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Selleck's Zafirlukast has been cited by 8 publications
| Inhibition of CysLTR1 reduces the levels of aggregated proteins in retinal pigment epithelial cells [ Sci Rep, 2023, 13(1):13239] | PubMed: 37580467 |
| Inhibition of CysLTR1 reduces the levels of aggregated proteins in retinal pigment epithelial cells [ Sci Rep, 2023, 13(1):13239] | PubMed: 37580467 |
| Cysteinyl leukotriene receptor 1 is a potent regulator of the endosomal-lysosomal system in the ARPE-19 retinal pigment epithelial cell line [ Traffic, 2023, 24(4):177-189] | PubMed: 36704929 |
| Zafirlukast Induces VHL- and HIF-2α-Dependent Oxidative Cell Death in 786-O Clear Cell Renal Carcinoma Cells [ Int J Mol Sci, 2022, 23(7)3567] | PubMed: 35408930 |
| Development of potent and selective inhibitors targeting the papain-like protease of SARS-CoV-2 [ Cell Chem Biol, 2021, S2451-9456(21)00213-0] | PubMed: 33979649 |
| Chronobiological activity of cysteinyl leukotriene receptor 1 during basal and induced autophagy in the ARPE-19 retinal pigment epithelial cell line [ Aging (Albany NY), 2021, 13(24):25670-25693] | PubMed: 34919533 |
| Cysteinyl leukotriene receptor 1 modulates autophagic activity in retinal pigment epithelial cells [ Sci Rep, 2020, 10(1):17659] | PubMed: 33077798 |
| Pranlukast is a novel small molecule activator of the two-pore domain potassium channel TREK2. [ Biochem Biophys Res Commun, 2019, 520(1):35-40] | PubMed: 31564414 |
RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.