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Z4152

Zafirlukast

≥98% (HPLC), CysLT1 receptor antagonist, solid

Synonym(s):

N-[3-[[2-Methoxy-4-[[[(2-methylphenyl)sulfonyl]amino]carbonyl]phenyl]methyl]-1-methyl-1H-indol-5-yl]carbamic acid cyclopentyl ester

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10 mg
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$107.00
50 mg
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$393.00
$334.05

About This Item

Empirical Formula (Hill Notation):
C31H33N3O6S
CAS Number:
107753-78-6
Molecular Weight:
575.68
UNSPSC Code:
12352200
PubChem Substance ID:
329831612
NACRES:
NA.77
MDL number:
MFCD00864775
Assay:
≥98% (HPLC)
Form:
solid

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Product Name

Zafirlukast, ≥98% (HPLC)

Quality Segment

assay

≥98% (HPLC)

form

solid

solubility

DMSO: ≥28 mg/mL

originator

AstraZeneca

storage temp.

room temp

SMILES string

COc1cc(ccc1Cc2cn(C)c3ccc(NC(=O)OC4CCCC4)cc23)C(=O)NS(=O)(=O)c5ccccc5C

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)

InChI key

YEEZWCHGZNKEEK-UHFFFAOYSA-N

Gene Information

human ... CYSLTR1(10800)

Application

Zafirlukast has been used to stimulate pancreatic β cell line (MIN6) and pancreatic islets for insulin secretion assay. It may be used as an adenosine triphosphate-binding cassette transporter (ABCG2) inhibitor in MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] cytotoxicity assay in human embryonic kidney cells (HEK293) and in Kirby-Bauer disc diffusion assays, bactericidal activity and minimal inhibitory concentration (mIC) assay against M. smegmatis

Biochem/physiol Actions

Zafirlukast is a potent subtype specific CysLT1 receptor antagonist; antiasthmatic.
Zafirlukast is a potent subtype specific cysteinyl leukotriene type 1 receptor (CysLT1) antagonist; antiasthmatic. Zafirlukast has over 1000-fold selectivity for CysLT1, one of two receptors for cysteinyl leukotrienes LTC4, LTD4, and LTE4, which are important mediators of human bronchial asthma.
Zafirlukast plays a key role in alleviating mucus and airway constriction in asthma based inflammatory response. It regulates pancreatic β cells for the secretion of insulin and this functionality is interlinked to the calcium based phosphorylation of the Ca2+/calmodulin-dependent protein kinase II (CaMKII) and protein kinase B (AKT). Zafirlukast has inhibitory potential on ATP-binding cassette (ABC) transporters and reverses the multidrug resistance function of ATP-binding cassette super-family G member 2 (ABCG2). Zafirlukast inhibits mycobacterial nucleoid-associated protein Lsr2 and halts the growth of Mycobacteria.

Features and Benefits

This compound is featured on the Leukotriene Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
This compound was developed by AstraZeneca. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

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This Item
C6239
Zafirlukast ≥98% (HPLC)

Sigma-Aldrich

Z4152

Zafirlukast

Cinalukast ~98% (HPLC)

Sigma-Aldrich

C6239

Cinalukast

description

≥98% (HPLC)

description

~98% (HPLC)

assay

≥98% (HPLC)

assay

~98% (HPLC)

form

solid

form

solid

Quality Level

100

Quality Level

100

storage temp.

room temp

storage temp.

2-8°C

solubility

DMSO: ≥28 mg/mL

solubility

DMSO: >10 mg/mL, H2O: insoluble

originator

AstraZeneca

originator

Roche

Hazard Codes

H413

Precautionary Statements

P273 - P501

Hazard Classifications

Aquatic Chronic 4

Storage Class

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable

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