WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 318990
CAS#: 107753-78-6
Description: Zafirlukast is an oral leukotriene receptor antagonist (LTRA) for the maintenance treatment of asthma, often used in conjunction with an inhaled steroid and/or long-acting bronchodilator. It is available as a tablet and is usually dosed twice daily. Another leukotriene receptor antagonist is montelukast (Singulair), taken once daily. Zileuton (Zyflo), also used in the treatment of asthma via its inhibition of 5-lipoxygenase, is taken four times per day. Zafirlukast blocks the action of the cysteinyl leukotrienes on the CysLT1 receptors, thus reducing constriction of the airways, build-up of mucus in the lungs and inflammation of the breathing passages.
MedKoo Cat#: 318990
Name: Zafirlukast
CAS#: 107753-78-6
Chemical Formula: C31H33N3O6S
Exact Mass: 575.20901
Molecular Weight: 575.68
Elemental Analysis: C, 64.68; H, 5.78; N, 7.30; O, 16.67; S, 5.57
Synonym: ICI-204219; ICI204219; ICI 204219; ICI-204,219; ICI 204,219; ICI204,219; Zafirlukast; brand names Accolate, Accoleit, and Vanticon.
IUPAC/Chemical Name: Cyclopentyl 3-{2-methoxy-4-[(o-tolylsulfonyl)carbamoyl]benzyl}-1-methyl-1H-indol-5-ylcarbamate
InChi Key: YEEZWCHGZNKEEK-UHFFFAOYSA-N
InChi Code: InChI=1S/C31H33N3O6S/c1-20-8-4-7-11-29(20)41(37,38)33-30(35)22-13-12-21(28(17-22)39-3)16-23-19-34(2)27-15-14-24(18-26(23)27)32-31(36)40-25-9-5-6-10-25/h4,7-8,11-15,17-19,25H,5-6,9-10,16H2,1-3H3,(H,32,36)(H,33,35)
SMILES Code: 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
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 575.68 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
1: Chen CF, Lv Y, Zhang HP, Wang G. Does zafirlukast reduce future risk of asthma exacerbations in adults? Systematic review and meta-analysis. Multidiscip Respir Med. 2014 May 28;9(1):30. doi: 10.1186/2049-6958-9-30. eCollection 2014. Review. PubMed PMID: 24936302; PubMed Central PMCID: PMC4059702.
2: Murata Y, Sugimoto O. [Zafirlukast (Accolate): a review of its pharmacological and clinical profile]. Nihon Yakurigaku Zasshi. 2002 Apr;119(4):247-58. Review. Japanese. PubMed PMID: 11979731.
3: Dekhuijzen PN, Koopmans PP. Pharmacokinetic profile of zafirlukast. Clin Pharmacokinet. 2002;41(2):105-14. Review. PubMed PMID: 11888331.
4: Dunn CJ, Goa KL. Zafirlukast: an update of its pharmacology and therapeutic efficacy in asthma. Drugs. 2001;61(2):285-315. Review. PubMed PMID: 11270943.
5: Montelukast and zafirlukast in asthma. Drug Ther Bull. 1998 Sep;36(9):65-8. Review. PubMed PMID: 10194869.
6: Calhoun WJ. Summary of clinical trials with zafirlukast. Am J Respir Crit Care Med. 1998 Jun;157(6 Pt 2):S238-45; discussion S245-8. Review. PubMed PMID: 9647606.
7: Holloway J, Ferriss J, Groff J, Craig TJ, Klinek M. Churg-Strauss syndrome associated with zafirlukast. J Am Osteopath Assoc. 1998 May;98(5):275-8. Review. Erratum in: J Am Osteopath Assoc 1998 Dec;98(12):676. Klinik M [corrected to Klinek M]. PubMed PMID: 9615559.
8: Adkins JC, Brogden RN. Zafirlukast. A review of its pharmacology and therapeutic potential in the management of asthma. Drugs. 1998 Jan;55(1):121-44. Review. PubMed PMID: 9463793.
9: Hendeles L, Marshik PL. Zafirlukast for chronic asthma: convenient and generally safe, but is it effective? Ann Pharmacother. 1997 Sep;31(9):1084-6. Review. PubMed PMID: 9296252.
10: Kelloway JS. Zafirlukast: the first leukotriene-receptor antagonist approved for the treatment of asthma. Ann Pharmacother. 1997 Sep;31(9):1012-21. Review. PubMed PMID: 9296243.
11: Spector SL. Management of asthma with zafirlukast. Clinical experience and tolerability profile. Drugs. 1996;52 Suppl 6:36-46. Review. PubMed PMID: 8941502.
