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

Zafirlukast (Synonyms: ICI 204219)

Cat. No.: HY-17492 Purity: 99.90%
Handling Instructions

Zafirlukast is a potent orally active leukotriene D4 (LTD4) receptor antagonist.

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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10 mM * 1 mL in DMSO USD 112 In-stock
Estimated Time of Arrival: December 31
100 mg USD 102 In-stock
Estimated Time of Arrival: December 31
500 mg USD 456 In-stock
Estimated Time of Arrival: December 31
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Description

Zafirlukast is a potent orally active leukotriene D4 (LTD4) receptor antagonist.

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].

Clinical Trial
Molecular Weight

575.68

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
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
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: ≥ 2.5 mg/mL (4.34 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.34 mM); Clear solution

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

Purity: 99.90%

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Keywords:

ZafirlukastICI 204219ICI204219ICI-204219Leukotriene ReceptorInhibitorinhibitorinhibit

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Zafirlukast
Cat. No.:
HY-17492
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