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Chemical Structure| 103177-37-3 Chemical Structure| 103177-37-3

Structure of Pranlukast
CAS No.: 103177-37-3

Chemical Structure| 103177-37-3

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Pranlukast is a selective CysLT1 receptor antagonist with high affinity for the CysLT1 receptor, with an IC50 value of 0.5 nM. Pranlukast has anti-allergic and anti-asthmatic effects and can be used in research on allergic diseases and asthma.

Synonyms: ONO-1078; ONO-RS-411; SB 205312

4.5 *For Research Use Only !

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Product Details of Pranlukast

CAS No. :103177-37-3
Formula : C27H23N5O4
M.W : 481.50
SMILES Code : O=C(NC1=C2C(C(C=C(C3=NN=NN3)O2)=O)=CC=C1)C4=CC=C(OCCCCC5=CC=CC=C5)C=C4
Synonyms :
ONO-1078; ONO-RS-411; SB 205312
MDL No. :MFCD00864631
InChI Key :NBQKINXMPLXUET-UHFFFAOYSA-N
Pubchem ID :4887

Safety of Pranlukast

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H315-H319-H228
Precautionary Statements:P240-P210-P241-P264-P280-P302+P352-P370+P378-P337+P313-P305+P351+P338-P362+P364-P332+P313
Class:4.1
UN#:1325
Packing Group:

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
HepG2-NTCPsec+ 4.3 μM 6 days Pranlukast inhibited HBV preS1 binding JHEP Rep. 2021 Apr 30;3(4):100296.
E. coli BL21(DE3) 0.001 μM 24 h Increased extracellular GALNS activity by 1.7-fold. J Med Chem. 2019 Jul 11;62(13):6175-6189.
Pichia pastoris 0.001 μM 48 h Increased GALNS activity up to 5.0-fold. J Med Chem. 2019 Jul 11;62(13):6175-6189.
P. falciparum D10 parasites 50 μM–98 nM 72 h To evaluate the effect of Pranlukast and its analogues on parasite growth, results showed that Pranlukast has weak inhibitory activity on parasite growth falciparum reticulocyte binding-like homologue 5 protein. Int J Parasitol Drugs Drug Resist.
P. falciparum 3D7 parasites 50 μM–98 nM 72 h To evaluate the effect of Pranlukast and its analogues on parasite growth, results showed that Pranlukast has weak inhibitory activity on parasite growth falciparum reticulocyte binding-like homologue 5 protein. Int J Parasitol Drugs Drug Resist.
HEK293 cells 0.001 μM 48 h Increased intracellular and extracellular GALNS activity by 1.3-fold and 1.8-fold, respectively. J Med Chem. 2019 Jul 11;62(13):6175-6189.
MCF-7 cells 50 μM To evaluate the effect of Pranlukast on MCF-7 cells, results showed that Pranlukast did not affect the adhesion of MCF-7 cells to laminin. Drug Des Devel Ther. 2020 May 12;14:1799-1811.
MDA-MB-231 cells 9.5 μM 24 h To evaluate the effect of Pranlukast on breast cancer stem cells, results showed that Pranlukast significantly reduced mammosphere formation in MDA-MB-231 cells. Drug Des Devel Ther. 2020 May 12;14:1799-1811.
Primary rat oligodendrocyte precursor cells 10 µM 5 min Pranlukast treatment effectively elevated intracellular cAMP levels. J Neurosci. 2016 Oct 12;36(41):10560-10573.
Primary rat oligodendrocyte precursor cells 10 µM 24 h Pranlukast ameliorated the deleterious effect of LPC on cell viability, whereas the Gpr17 agonist MDL29951 augmented the effect of LPC. J Neurosci. 2016 Oct 12;36(41):10560-10573.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Myocardial ischemia-reperfusion injury model Intraperitoneal injection 0.5 mg/kg Once daily for 3 days Pranlukast ameliorated myocardial ischemia-reperfusion injury by inhibiting NETosis, particularly in ALDH2 knockout mice. Eur Heart J. 2024 May 13;45(18):1662-1680
Mice Acute and chronic tuberculosis infection models Oral 40 mg/kg 5 times a week for 4 weeks Pranlukast was more effective in the acute infection model than in the chronic infection model, significantly reducing bacterial load in the lungs and spleen, and promoting lung tissue repair. Front Immunol. 2024 May 2;15:1347045
Nude mice Breast cancer xenograft model Injection into the mammary fat pad 50 μM Single injection, lasting 36 days To evaluate the effect of Pranlukast on breast cancer stem cell tumorigenicity in vivo, results showed that Pranlukast significantly reduced the number of tumor-initiating cells. Drug Des Devel Ther. 2020 May 12;14:1799-1811.
Mice LPC-induced demyelination model Intraperitoneal injection 0.1 mg/kg Every 12 hours for 7 days Pranlukast treatment promoted remyelination after LPC-induced demyelination. J Neurosci. 2016 Oct 12;36(41):10560-10573.
Mice LPS-induced depressive-like behavior model Oral 0.3 mg/kg or 0.6 mg/kg Single administration Pranlukast significantly suppressed LPS-induced depressive-like behaviors in mice, reducing immobility time in the TST and latency to feed in the NSF test, without affecting locomotor activity. Acta Pharmacol Sin. 2017 Apr;38(4):477-487

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00127647 Rhinitis, Allergic, Seasonal Phase 3 Completed - -
NCT01539304 Perennial Allergic Rhinitis Phase 3 Completed - Korea, Republic of ... More >> Seoul National University Hodpital Seoul, Korea, Republic of Less <<
NCT00410735 Chronic Sinusitis Phase 3 Completed - Japan ... More >> Chubu region Chubu, Japan Hokuriku region Hokuriku, Japan Kanto region Kanto, Japan Kinki region Kinki, Japan Kyushu region Kyushu, Japan Tohoku region Tohoku, Japan Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.08mL

0.42mL

0.21mL

10.38mL

2.08mL

1.04mL

20.77mL

4.15mL

2.08mL

References

 

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