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Zafirlukast

SKU: orb1300514

Description

Zafirlukast is a potent and selective antagonist of the leukotriene D4 receptor (IC50=0.6 µM). This orally active compound is used in asthma research for its anti-inflammatory properties and has been investigated in both in vitro binding assays and in vivo models of airway hyperresponsiveness.

Research Area

Pharmacology & Drug Discovery

Images & Validation

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Zafirlukast

Key Properties

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CAS Number107753-78-6
MW575.68
Purity99.83% (May vary between batches)
FormulaC31H33N3O6S
SMILESCOc1cc(ccc1Cc1cn(C)c2ccc(NC(=O)OC3CCCC3)cc12)C(=O)NS(=O)(=O)c1ccccc1C
TargetLeukotriene Receptor
SolubilityEthanol:< 1 mg/mL (insoluble or slightly soluble);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:105 mg/mL (182.39 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (6.95 mM)

Bioactivity

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In Vivo
METHODS: To detect anti-tumor activity in vivo, THZ1 (10 mg/kg) was injected intravenously twice daily for 28 days into NU/NU mice bearing MYCN-amplified human NB xenografts. RESULTS: THZ1 inhibited tumor growth in the human MYCN-amplified NB mouse model. METHODS: To detect the antitumor activity in vivo, THZ1 (10 mg/kg) was injected intraperitoneally into NSG mice bearing KYSE510 tumors twice daily for 24 days. RESULTS: THZ1 inhibited the growth of KYSE510 xenografts and suppressed lung metastasis in the NSG mouse model.
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In Vitro
METHODS: Loucy cells were treated with THZ1 (0.8-500 nM) for 4 h. Binding was detected by LanthaScreen Eu Kinase Binding assay. RESULTS: THZ1 showed time-dependent inhibition of CDK7 in vitro and covalent binding of intracellular CDK7. METHODS: NSCLC cell lines H1299, A549 and H292 were treated with THZ1 (10-10000 nM) for 48 h. Cell viability was measured by crystal violet assay. RESULTS: THZ1 dose-dependently inhibited the migration and proliferation of NSCLC cells.
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Storage & Handling

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Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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inhibit, leukotriene receptor, Leukotriene Receptor, LeukotrieneReceptor, ICI204219, ICI-204219, ICI 204219, Inhibitor, Accolate, Vanticon, Zafirlukast

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Quality Guarantee

Quality Guarantee

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Compound Identifiers

PubChem CID
5717 ↗

Key Properties

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No computed properties available.

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Zafirlukast (orb1300514)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

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10 mg
$ 70.00
25 mg
$ 90.00
1 ml x 10 mM (in DMSO)
$ 100.00
50 mg
$ 110.00
100 mg
$ 140.00
500 mg
$ 320.00
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