1. GPCR/G Protein
  2. Leukotriene Receptor
  3. Zafirlukast

Zafirlukast  (Synonyms: ICI 204219)

Cat. No.: HY-17492 Purity: 99.89%
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

Zafirlukast Chemical Structure

CAS No. : 107753-78-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of Zafirlukast:

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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

 

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.
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
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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

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%

References
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

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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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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Zafirlukast
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