Zafirlukast (Synonyms: ICI 204219)

Name: Zafirlukast
Brand: MedChemExpress
SKU: HY-17492
Rating: 5.0 (3 reviews)

Cat. No.: HY-17492 Purity: 99.87%: Data Sheet
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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.

CAS No. : 107753-78-6

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
100 mg	In-stock	Estimated Time of Arrival: December 31
500 mg	In-stock	Estimated Time of Arrival: December 31
1 g	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of Zafirlukast:

3 Publications Citing Use of MCE Zafirlukast

Bio/Physico-chemical Assay

: 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).

: 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.

: 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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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

Zafirlukast (ICI 204219) is a potent orally active leukotriene D₄ (LTD₄) receptor antagonist. Zafirlukast shows anti-asthmatic, anti-inflammatory and anti-bacterial effects.

IC₅₀ & Target^[1]

LTD₄

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	18.1 μM Compound: 34	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	10.1039/C5MD00278H
HEK-293T	IC₅₀	7397 nM Compound: zafirlukast	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	[PMID: 26200813]
HEK293	IC₅₀	0.014 μM Compound: Accolate	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	[PMID: 26985325]
HEK293	IC₅₀	1.3 μM Compound: zafirlukast	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	[PMID: 23241029]
HEK293	IC₅₀	58 μM Compound: Accolate	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	[PMID: 26985325]
HEK293	IC₅₀	7.6 μM Compound: zafirlukast	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	[PMID: 23241029]
HEK293	IC₅₀	9.7 μM Compound: zafirlukast	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	[PMID: 23241029]
HGC-27	IC₅₀	44 μM Compound: 1; ZAF	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	[PMID: 36622814]
HepG2	EC₅₀	14.1 μM Compound: Zafirlukast	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	[PMID: 20966043]
HepG2	EC₅₀	58.4 μM Compound: Zafirlukast	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	[PMID: 20966043]
HepG2	EC₅₀	9.5 μM Compound: Zafirlukast	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	[PMID: 20966043]
U-937	IC₅₀	0.001 μM Compound: 1	Compound was evaluated for influx of calcium mobilization in human U937 cells Compound was evaluated for influx of calcium mobilization in human U937 cells	[PMID: 9873435]
U-937	IC₅₀	0.001 μM Compound: 1	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	[PMID: 9934474]
U-937	IC₅₀	1 nM Compound: 1	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	[PMID: 9873560]
U-937	IC₅₀	1 nM Compound: Zafirlukast	In vitro blocking of extracellular calcium mobilization in human U937 cells In vitro blocking of extracellular calcium mobilization in human U937 cells	[PMID: 10509933]
U2OS	IC₅₀	6.5 μM Compound: Zafirlukast	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	[PMID: 31439379]

In Vivo

Zafirlukast is a peptidyl leukotriene antagonist and inhibitor of LTD₄. After 13 weeks of exposure, the yield of lung tumors is significantly decreased by both dose levels of Zafirlukast (270 and 540 mg/kg), the high dose of Zileuton (1200 mg/kg), and the combinations containing 600 mg/kg Zileuton with either Zafirlukast or MK-866. The efficacy of the combination containing Zileuton and Zafirlukast to prevent lung tumors is not significantly different from the efficacy of either inhibitor administered alone. Although when administered alone at the dose level in their combination, neither Zileuton or MK-886 prevents lung tumors; the combination containing them does significantly prevent tumors. In contrast, the combination containing Zafirlukast and MK-886 does not reduce the yield of tumors, whereas Zafirlukast administered alone does significantly reduce the yield of tumors^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

575.68

Formula

C₃₁H₃₃N₃O₆S

CAS No.

107753-78-6

Appearance

Solid

Color

Off-white to pink

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (3.61 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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mg/kg

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Dosing volume
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μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.89%

Select Batch:

Data Sheet (275 KB) SDS (597 KB)

COA (249 KB) LCMS (95 KB)

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]

Animal Administration
^[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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

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

Zafirlukast Related Classifications

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Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Zafirlukast107753-78-6ICI 204219ICI204219ICI-204219Leukotriene ReceptorInhibitorinhibitorinhibit

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Zafirlukast (Synonyms: ICI 204219)

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Other Forms of Zafirlukast:

Zafirlukast Related Antibodies

3 Publications Citing Use of MCE Zafirlukast

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Complete Stock Solution Preparation Table

Zafirlukast Related Classifications

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