| Size | Price | Stock | Qty |
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| 100mg |
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| 500mg |
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| 1g |
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| 2g |
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| 5g |
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Purity: ≥98%
Pranlukast is a potent, selective and competitive antagonist of cysteinyl leukotriene receptor-1 (CysLT1) Pranlukast with Kis of 0.63±0.11, 0.99±0.19, and 5640±680 nM for inhibiting [3H]LTE4, [3H]LTD4, and [3H]LTC4 bindings to lung membranes, respectively. It opposes or lessens bronchospasm, which is primarily brought on in asthmatics by an allergic reaction to allergens that they unintentionally or mistakenly touch. They are microvascular permeability enhancers, bronchoconstrictors, and coronary artery vasoconstrictors. CysLT1 and CysLT2, two G protein-coupled receptors, are responsible for transducing their biological effects.
| Targets |
LTE4 ( Ki = 0.63 nM ); LTD4 ( Ki = 0.99 nM ); LTC4 ( Ki = 5640 nM )
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| ln Vitro |
Pranlukast reduces NF-kappa B activation in 1.3% DMSO-differentiated Jurkat and U-937 cells by approximately 30% and 40%, respectively. In 1.3% DMSO-differentiated U-937 and Jurkat cells, pranlukast and MK-571 inhibit NF-kappa B activation in a dose-related fashion. The production of IL-6 in PBMC stimulated by LPS is inhibited by pranlukast and MK-571 by approximately 65% and 15%, respectively. (Source: ) 10 mM LTD4-evoked 35SO4 output is significantly inhibited by both zafirlukast and pranlukast in a concentration-dependent manner; the maximal inhibitions are 83% and 78% at 10 mM zafirlukast and 0.3 mM and 0.6 mM, respectively, for both drugs. Pranlukast (0.5 microM) causes a parallel rightward shift in the LTD4 concentration-response curve with a pKB.[3] The ovalbumin-induced secretion in the tracheae of sensitized guinea pigs is markedly suppressed by either pranlukast (5 microM) or zafirlukast (65%), respectively. In [2] Pranlukast also inhibits NF-kappaB activation induced by phorbol 12-myristate 13-acetate (PMA). Pranlukast also significantly inhibits LPS-induced MUC2 mRNA expression by reverse transcription-polymerase chain reaction (RT-PCR) analysis in NCI-H292 cells. Pranlukast also inhibits LPS-induced MUC2 gene expression in HM3-MUC2 cells.[3]
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| ln Vivo |
Pranlukast increases neuron densities in the cortex and hippocampal CA1 region in the mice's ischemic hemispheres and dramatically decreases the volume of lesion. Pranlukast also significantly lessens the scar wall's thickness in mice's ischemic hemispheres.[4]
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| Cell Assay |
Penicillin (100 U/mL), Streptomycin (100 mg/mL), and 10% heat-inactivated fetal calf serum are added to Dulbecco's modified Eagle's medium (DMEM) for the culture of EA.hy926 cells. The experiments take place 24 hours after the cells are seeded. OGD is executed. In short, the original medium is taken out, and the cells are then put in fresh glucose-free Earle's balanced salt solution (EBSS) after being twice washed with it. After that, cultures are kept in an incubator with 5% CO2 and 95% N2 at 37°C for two to eight hours. Normal conditions are maintained for control cultures in EBSS containing glucose. The culture is supplemented with 10 μM Pyrrolidine dithiocarbamate (PDTC), 10 μM Zileuton, a 5-LOX inhibitor, or 10 μM Pranlukast 30 minutes prior to OGD exposure and kept there throughout OGD[2].
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| Animal Protocol |
Mice: The mice used are male ddY mice. Every mouse that is used is between 7 and 8 weeks old. Mice are given endotoxin shock. To summarize, 24 hours prior to LPS challenge, intraperitoneal (i.p.) injection of CAR (5 mg in 0.5 mL of physiological saline) is administered as a priming agent. The inducing agent, LPS (50 p.g in 0.5 mL of physiological saline), is administered intravenously into the tail vein. Mice are given AA-861, pranlukast (40, 20, and 10 mmol/kg), ethanol, saline, or DMSO subcutaneously (s.c.) in a volume of 1 mL into their backs 30 minutes prior to the LPS provocation. Since peritonitis was caused by CAR i.p. pretreatment, both medications are injected subcutaneously. Before the LPS challenge, 2×105 U of rabbit anti-TNF-a antibody or rabbit normal serum in 0.2 mL is injected intravenously (i.v.) to investigate the function of endogenous TNF in CAR-pretreated mice[3].
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| References |
| Molecular Formula |
C27H23N5O4
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|---|---|
| Molecular Weight |
481.5026
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| Exact Mass |
481.18
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| Elemental Analysis |
C, 67.35; H, 4.81; N, 14.54; O, 13.29
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| CAS # |
103177-37-3
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| Related CAS # |
Pranlukast hemihydrate; 50821-03-7; Pranlukast-d4; 2713172-43-9
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| Appearance |
Solid powder
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| SMILES |
C1=CC=C(C=C1)CCCCOC2=CC=C(C=C2)C(=O)NC3=CC=CC4=C3OC(=CC4=O)C5=NNN=N5
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| InChi Key |
NBQKINXMPLXUET-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H23N5O4/c33-23-17-24(26-29-31-32-30-26)36-25-21(23)10-6-11-22(25)28-27(34)19-12-14-20(15-13-19)35-16-5-4-9-18-7-2-1-3-8-18/h1-3,6-8,10-15,17H,4-5,9,16H2,(H,28,34)(H,29,30,31,32)
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| Chemical Name |
N-[4-oxo-2-(2H-tetrazol-5-yl)chromen-8-yl]-4-(4-phenylbutoxy)benzamide
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| Synonyms |
Ono-1078; ONO 1078; ONO-1078; ONO-RS 411; ONO-RS-411; SB 205312; Pranlukast
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 11~33.3 mg/mL (22.8~69.2 mM)
H2O: ~0.7 mg/mL (~1.4 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.75 mg/mL (5.71 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.75 mg/mL (5.71 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 27.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 5% DMSO+ 95% Corn oil: 0.6mg/ml (1.25mM) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0768 mL | 10.3842 mL | 20.7684 mL | |
| 5 mM | 0.4154 mL | 2.0768 mL | 4.1537 mL | |
| 10 mM | 0.2077 mL | 1.0384 mL | 2.0768 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00410735 | Completed | Drug: Placebo Drug: Pranlukast hydrate |
Chronic Sinusitis | Ono Pharmaceutical Co. Ltd | December 2006 | Phase 3 |
| NCT00127647 | Completed | Drug: montelukast sodium Drug: Comparator: pranlukast |
Rhinitis, Allergic, Seasonal | Organon and Co | November 2004 | Phase 3 |
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