Pranlukast (Synonyms: ONO-1078)

Name: Pranlukast
Brand: MedChemExpress
SKU: HY-B0290
Rating: 5.0 (3 reviews)

Art. -Nr.: HY-B0290 Reinheit: 99.61%: Data Sheet
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Handling Instructions
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Pranlukast is a highly potent, selective and competitive antagonist of peptide leukotrienes. Pranlukast inhibits [³H]LTE₄, [³H]LTD₄, and [³H]LTC₄ bindings to lung membranes with K_is of 0.63±0.11, 0.99±0.19, and 5640±680 nM, respectively.

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CAS. Nr. : 103177-37-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	Auf Lager	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	Auf Lager	Estimated Time of Arrival: December 31
Solid
100 mg	Auf Lager	Estimated Time of Arrival: December 31
500 mg	Auf Lager	Estimated Time of Arrival: December 31
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Based on 3 publication(s) in Google Scholar

Other Forms of Pranlukast:

Pranlukast hemihydrate In-stock
Pranlukast (Standard) In-stock
Pranlukast-d₄ Angebot einholen

3 Publications Citing Use of MCE Pranlukast

Cell Proliferation/Viability Assay

: Pranlukast purchased from MedChemExpress. Usage Cited in: J Neurosci. 2016 Oct 12;36(41):10560-10573. [Abstract]; The inhibition of Epac1 activity by ESI-09 reduces oligodendrocyte maturation.

: Pranlukast purchased from MedChemExpress. Usage Cited in: J Neurosci. 2016 Oct 12;36(41):10560-10573. [Abstract]; The inhibition of PKA signaling with PKA inhibitor H89 reduces cell viability observed after Pranlukast treatment.

Spezialitätsempfehlungen

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Alle Leukotriene Receptor Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen

LTB₄ LTC₄/CysLT₂ LTD₄/CysLT₁ LTE₄

Alle Endogenous Metabolite Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen

Human Endogenous Metabolite Microbial Metabolite

Biologische Aktivität
Protokoll
Reinheit & Dokumentation
Verweise
Kundenbewertung

Beschreibung

IC₅₀ & Target^[1]

LTE₄

0.63 nM (Ki)

LTD₄

0.99 nM (Ki)

LTC₄

5640 nM (Ki)

Cellular Effect

Cell Line	Type	Value	Description	References
U-937	IC₅₀	1 1 Compound: Pranlukast	In vitro blocking of extracellular calcium mobilization in human U937 cells In vitro blocking of extracellular calcium mobilization in human U937 cells	[PMID: 10509933]
HEK-293T	IC₅₀	3620 1 Compound: pranlukast	Antagonist activity at human CysLT2 expressed in HEK293T cells assessed as inhibition of LTC4-induced effect preincubated for 30 mins prior to LTC4 addition by Aequorin luminescence assay Antagonist activity at human CysLT2 expressed in HEK293T cells assessed as inhibition of LTC4-induced effect preincubated for 30 mins prior to LTC4 addition by Aequorin luminescence assay	[PMID: 26200813]
HeLa	EC₅₀	15 3 Compound: Pranlukast	Partial agonist activity at human full-length FXR expressed in human HeLa cells co-expressing pSG5-RXR measured after 24 hrs by dual-glo luciferase reporter gene assay Partial agonist activity at human full-length FXR expressed in human HeLa cells co-expressing pSG5-RXR measured after 24 hrs by dual-glo luciferase reporter gene assay	[PMID: 31188588]
HeLa	EC₅₀	15 3 Compound: Pranlukast	Partial agonist activity at human full-length FXR expressed in human HeLa cells co-expressing pSG5-RXR measured after 24 hrs by dual-glo luciferase reporter gene assay Partial agonist activity at human full-length FXR expressed in human HeLa cells co-expressing pSG5-RXR measured after 24 hrs by dual-glo luciferase reporter gene assay	[PMID: 31188588]
HEK-293T	IC₅₀	3620 1 Compound: pranlukast	Antagonist activity at human CysLT2 expressed in HEK293T cells assessed as inhibition of LTC4-induced effect preincubated for 30 mins prior to LTC4 addition by Aequorin luminescence assay Antagonist activity at human CysLT2 expressed in HEK293T cells assessed as inhibition of LTC4-induced effect preincubated for 30 mins prior to LTC4 addition by Aequorin luminescence assay	[PMID: 26200813]
HEK-293T	IC₅₀	3620 1 Compound: pranlukast	Antagonist activity at human CysLT2 expressed in HEK293T cells assessed as inhibition of LTC4-induced effect preincubated for 30 mins prior to LTC4 addition by Aequorin luminescence assay Antagonist activity at human CysLT2 expressed in HEK293T cells assessed as inhibition of LTC4-induced effect preincubated for 30 mins prior to LTC4 addition by Aequorin luminescence assay	[PMID: 26200813]
U-937	IC₅₀	0.001 3 Compound: 2	Compound was evaluated for influx of calcium mobilization in human U937 cells Compound was evaluated for influx of calcium mobilization in human U937 cells	[PMID: 9873435]
HeLa	EC₅₀	15 3 Compound: Pranlukast	Partial agonist activity at human full-length FXR expressed in human HeLa cells co-expressing pSG5-RXR measured after 24 hrs by dual-glo luciferase reporter gene assay Partial agonist activity at human full-length FXR expressed in human HeLa cells co-expressing pSG5-RXR measured after 24 hrs by dual-glo luciferase reporter gene assay	[PMID: 31188588]
U-937	IC₅₀	0.001 3 Compound: 2	Compound was tested for its ability to inhibit calcium influx in human U937 cells Compound was tested for its ability to inhibit calcium influx in human U937 cells	[PMID: 9934474]
U-937	IC₅₀	0.001 3 Compound: 2	Compound was evaluated for influx of calcium mobilization in human U937 cells Compound was evaluated for influx of calcium mobilization in human U937 cells	[PMID: 9873435]
U-937	IC₅₀	0.001 3 Compound: 2	Compound was tested for its ability to inhibit calcium influx in human U937 cells Compound was tested for its ability to inhibit calcium influx in human U937 cells	[PMID: 9934474]
U-937	IC₅₀	1 1 Compound: Pranlukast	In vitro blocking of extracellular calcium mobilization in human U937 cells In vitro blocking of extracellular calcium mobilization in human U937 cells	[PMID: 10509933]

In Vitro

In the radioligand binding assay, Pranlukast (ONO-1078) inhibits [³H]LTE₄, [³H]LTD₄, and [³H]LTC₄ bindings to lung membranes with K_is of 0.63±0.11, 0.99±0.19, and 5640±680 nM, respectively. The antagonism of Pranlukast against [³H]LTD₄ binding is competitive. In functional experiments, Pranlukast shows competitive antagonism against the LTC₄- and LTD₄-induced contractions of guinea pig trachea and lung parenchymal strips with a pA₂ range of 7.70 to 10.71. In the presence of an inhibitor of the bioconversion of LTC₄ to LTD₄, Pranlukast also antagonizes the LTC₄-induced contraction of guinea pig trachea (pA₂=7.78). Pranlukast significantly reverses the LTD₄-induced prolonged contraction without effect on the KCl- and BaCl₂-induced contractions of guinea pig trachea^[1]. Oxygen-glucose deprivation (OGD)-induced nuclear translocation of CysLT₁ receptors is inhibited by pretreatment with the CysLT₁ receptor antagonist Pranlukast (10 μM). Pranlukast protects endothelial cells against ischemia-like injury. The effects of the CysLT₁ receptor antagonist Pranlukast and the 5-lipoxygenase inhibitor Zileuton on translocation are also assessed. The results show that Pranlukast, but not Zileuton, inhibits the translocation of the CysLT₁ receptor 6 h after OGD^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Carrageenan (CAR, 5 mg per mouse) is injected i.p. 24 h before LPS (50 μg per mouse) is injected i.v. Various doses of Pranlukast (ONO-1078; 40, 20, and 10 mmol/kg), AA-861 (20, 10, and 5 mmol/kg), Indomethacin (40 mmollkg), and the controls are injected s.c. into mice 30 min before they are challenged with 50 p,g of LPS. The maximum soluble doses are 0.6 mmol/mL in 10% DMSO for AA-861 and 1.2 mmol/mL in 10% ethanol for Pranlukast. These solutions are used as the maximum doses for the treatments. The mortality of mice is significantly decreased in AA-861- Pranlukast-treated mice relative to that in the control mice. Pretreatment with CAR (5 mg i.p.) renders the mice more sensitive to the effect of LPS. Although the survival rate of mice treated with each solvent is 20% at 72 h after LPS (50 p,g per mouse) administration, s.c. treatment with AA-861 (20 mmol/kg) or Pranlukast (40 mmol/kg) significantly increases the survival rate after the LPS administration (AA-861, P<0.001; Pranlukast, P<0.01)^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Klinische Studie

Molekulargewicht

481.50

Formel

C₂₇H₂₃N₅O₄

CAS. Nr.

103177-37-3

Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=C2C(C(C=C(C3=NNN=N3)O2)=O)=CC=C1)C4=CC=C(OCCCCC5=CC=CC=C5)C=C4

Structure Classification

Initial Source

Endogenous metabolite

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 33.33 mg/mL (69.22 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner
Verdünnungsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.75 mg/mL (5.71 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.75 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.75 mg/mL (5.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Reinheit & Dokumentation

Purity: 99.61%

Select Batch:

Data Sheet (279 KB) SDS (393 KB)

COA (248 KB) HNMR (138 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

Verweise

[1]. Obata T, et al. In vitro antagonism of ONO-1078, a newly developed anti-asthma agent, against peptide leukotrienes in isolated guinea pig tissues. Jpn J Pharmacol. 1992 Nov;60(3):227-37. [Content Brief]

[2]. Fang SH, et al. Nuclear translocation of cysteinyl leukotriene receptor 1 is involved in oxygen-glucose deprivation-induced damage to endothelial cells. Acta Pharmacol Sin. 2012 Dec;33(12):1511-7. [Content Brief]

[3]. Ogata M, et al. Protective effects of a leukotriene inhibitor and a leukotriene antagonist on endotoxin-induced mortality in carrageenan-pretreated mice. Infect Immun. 1992 Jun;60(6):2432-7. [Content Brief]

Zellassay ^[2]	EA.hy926 cells are cultured in Dulbecco's modified Eagle's medium (DMEM), supplemented with 10% heat-inactivated fetal calf serum, Penicillin (100 U/mL) and Streptomycin (100 mg/mL). Experiments are conducted 24 h after cells are seeded. OGD is performed. Briefly, the original medium is removed; the cells are washed twice with glucose-free Earle's balanced salt solution (EBSS) and placed in fresh glucose-free EBSS. Cultures are then placed in an incubator containing 5% CO₂ and 95% N₂ at 37°C for 2 to 8 h. Control cultures are maintained in glucose-containing EBSS under normal conditions. 10 μM Pranlukast, 10 μM Zileuton, a 5-LOX inhibitor or 10 μM Pyrrolidine dithiocarbamate (PDTC), is added to the culture 30 min before OGD exposure and maintained during OGD^[2]. MCE hat die Genauigkeit dieser Methoden nicht unabhängig bestätigt. Sie dienen nur als Referenz.
Tierverwaltung ^[3]	Mice^[3] Male ddY mice are used. All mice used are 7 to 8 weeks of age. Endotoxin shock is induced in mice. In brief, CAR (5 mg in 0.5 mL of physiological saline) is injected intraperitoneally (i.p.) as a priming agent 24 h before LPS challenge. LPS (50 p,g in 0.5 mL of physiological saline) is injected intravenously into the tail vein as an inducing agent. The indicated doses of AA-861, Pranlukast (40, 20, and 10 mmol/kg), saline, DMSO, or ethanol are administrated subcutaneously (s.c.) in a volume of 1 mL into the backs of mice 30 min before the LPS provocation. Both drugs are injected s.c., because CAR i.p. pretreatment caused peritonitis. To examine the role of endogenous TNF in CAR pretreated mice, 2×10⁵ U of rabbit anti-TNF-a antibody or normal serum of rabbit in 0.2 mL is injected intravenously (i.v.) before the LPS challenge^[3]. MCE hat die Genauigkeit dieser Methoden nicht unabhängig bestätigt. Sie dienen nur als Referenz.
Verweise	[1]. Obata T, et al. In vitro antagonism of ONO-1078, a newly developed anti-asthma agent, against peptide leukotrienes in isolated guinea pig tissues. Jpn J Pharmacol. 1992 Nov;60(3):227-37. [Content Brief] [2]. Fang SH, et al. Nuclear translocation of cysteinyl leukotriene receptor 1 is involved in oxygen-glucose deprivation-induced damage to endothelial cells. Acta Pharmacol Sin. 2012 Dec;33(12):1511-7. [Content Brief] [3]. Ogata M, et al. Protective effects of a leukotriene inhibitor and a leukotriene antagonist on endotoxin-induced mortality in carrageenan-pretreated mice. Infect Immun. 1992 Jun;60(6):2432-7. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.0768 mL	10.3842 mL	20.7684 mL	51.9211 mL
	5 mM	0.4154 mL	2.0768 mL	4.1537 mL	10.3842 mL
	10 mM	0.2077 mL	1.0384 mL	2.0768 mL	5.1921 mL
	15 mM	0.1385 mL	0.6923 mL	1.3846 mL	3.4614 mL
	20 mM	0.1038 mL	0.5192 mL	1.0384 mL	2.5961 mL
	25 mM	0.0831 mL	0.4154 mL	0.8307 mL	2.0768 mL
	30 mM	0.0692 mL	0.3461 mL	0.6923 mL	1.7307 mL
	40 mM	0.0519 mL	0.2596 mL	0.5192 mL	1.2980 mL
	50 mM	0.0415 mL	0.2077 mL	0.4154 mL	1.0384 mL
	60 mM	0.0346 mL	0.1731 mL	0.3461 mL	0.8654 mL

Pranlukast Related Classifications

Inflammation/Immunology

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Pranlukast103177-37-3ONO-1078ONO1078ONO 1078Leukotriene ReceptorEndogenous MetaboliteInhibitorinhibitorinhibit

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Pranlukast (Synonyms: ONO-1078)

Kundenbewertung

Other Forms of Pranlukast:

Pranlukast Related Antibodies

3 Publications Citing Use of MCE Pranlukast

Spezialitätsempfehlungen

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Alle Leukotriene Receptor Isoform-spezifische Produkte anzeigen:

Alle Endogenous Metabolite Isoform-spezifische Produkte anzeigen:

Biologische Aktivität

Protokoll

Reinheit & Dokumentation

Verweise

Kundenbewertung

Pranlukast Related Antibodies

Molaritätsrechner

Verdünnungsrechner

Complete Stock Solution Preparation Table

Pranlukast Related Classifications

Keywords:

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