Zafirlukast (Synonyms: ICI 204219)

Cat. No.: HY-17492 Purity: 99.90%: FAQs
Data Sheet SDS COA Handling Instructions

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.

Zafirlukast Chemical Structure

CAS No. : 107753-78-6

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Solution
10 mM * 1 mL in DMSO	USD 112	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL ready for reconstitution	USD 112	In-stock	Estimated Time of Arrival: December 31
Solid
100 mg	USD 102	In-stock	Estimated Time of Arrival: December 31
500 mg	USD 370	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Zafirlukast:

Zafirlukast-d₇ Get quote

2 Publications Citing Use of MCE Zafirlukast

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LTB₄ LTC₄ LTD₄/CysLT₁ LTE₄ CysLT₂ CysLT₁

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

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].

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

Clinical Trial

Molecular Weight

575.68

Appearance

Solid

Formula

C₃₁H₃₃N₃O₆S

CAS No.

107753-78-6

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)

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

*Please refer to the solubility information to select the appropriate solvent.

In Vivo:

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
2.

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

*All of the co-solvents are available by MCE.

Purity & Documentation

Purity: 99.90%

Select Batch:

Data Sheet (275 KB) SDS (393 KB)

COA (249 KB) LCMS (120 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]

Zafirlukast Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
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.

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Keywords:

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

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Zafirlukast (Synonyms: ICI 204219)

Customer Review

Other Forms of Zafirlukast:

Zafirlukast Related Antibodies

2 Publications Citing Use of MCE Zafirlukast

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•Related Screening Libraries:

•Related Small Molecules:

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View All Leukotriene Receptor Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Zafirlukast Related Classifications

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The dilution calculator equation

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