2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  3. Histamine Receptor Leukotriene Receptor Prostaglandin Receptor
  4. Quinotolast sodium

Quinotolast sodium  (Synonyms: FR71021)

Cat. No.: HY-U00027 Purity: 98.38%
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Quinotolast sodium in the concentration range of 1-100 μg/mL inhibits histamine, LTC4 and PGD2 release in a concentration-dependent manner.

For research use only. We do not sell to patients.

Quinotolast sodium Chemical Structure

Quinotolast sodium Chemical Structure

CAS No. : 101193-62-8

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1 mg USD 200 In-stock
5 mg USD 500 In-stock
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Quinotolast sodium Related Antibodies

Top Publications Citing Use of Products

View All Histamine Receptor Isoform Specific Products:

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H1 Receptor H2 Receptor H3 Receptor H4 Receptor Histamine Receptor

View All Leukotriene Receptor Isoform Specific Products:

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LTB4 LTC4/CysLT2 LTD4/CysLT1 LTE4

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DP EP FP IP TXA2/TP TXB2

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Quinotolast sodium in the concentration range of 1-100 μg/mL inhibits histamine, LTC4 and PGD2 release in a concentration-dependent manner.

IC50 & Target[1]

Histamine

 

LTC4

 

In Vitro

Quinotolast inhibits the release of histamine and the generation of leukotriene (LT) C4 and prostaglandin (PG) D2 from dispersed human lung cells. Quinotolast (100 μg/mL) significantly inhibits PGD2 and LTC4 release. Quinotolast inhibits PGD2 release by 100% and LTC4 release by 54%. The inhibitory effect of Quinotolast on histamine release from dispersed lung cells is largely independent of the preincubation period, no tachyphylaxis being observed. Quinotolast shows a significant inhibition of inflammatory mediators from human dispersed lung cells[1]. Quinotolast also shows strong inhibitory effects on histamine and peptide leukotrienes release from guinea pig lung fragments or mouse cultured mast cells. Quinotolast concentration-dependently inhibits pLTs release from cultured mast cells. The IC50 value for Quinotolast is 0.72 μg/mL[2].

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

Quinotolast sodium Related Antibodies
In Vivo

Quinotolast potently inhibits such type I allergic reactions as passive cutaneous anaphylaxis (PCA) and anaphylactic bronchoconstriction in rats by both intravenous and oral dosing. When Quinotolast is given i.v. to rats, Quinotolast, dose-dependently inhibits PCA. The doses of Quinotolast required to inhibit the reaction by 50% (ED50) is 0.0063 mg/kg. Given p.o., Quinotolast inhibits the reaction. ED50 value for Quinotolast is 0.0081 mg/kg. Although almost complete inhibition is observed with Quinotolast at a dose of 0.32 mg/kg, its effect is slightly attenuated at a dose of 1 mg/kg[2].

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

371.31

Formula

C17H12N6NaO3
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(NC1=NN=NN1)C2=CC(OC3=CC=CC=C3)=C4N(C2=O)C=CC=C4.[Na]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 115 mg/mL (309.71 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6932 mL 13.4658 mL 26.9317 mL
5 mM 0.5386 mL 2.6932 mL 5.3863 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: 5.75 mg/mL (15.49 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 5.75 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 (57.5 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% (20% SBE-β-CD in Saline)

    Solubility: 5.75 mg/mL (15.49 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 5.75 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 (57.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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.
Purity & Documentation
References
Cell Assay
[2]

Mast cells are obtained after the culture of bone marrow cells from the femurs of female BDF1 mice in the presence of conditioned medium from WEHI-3 cells containing interleukin 3. The cells are suspended with Tyrode's buffer (137 mM NaCI, 2.7 mM KC1, 1.8 mM CaCl2, 1 mM MgCl2, 0.4 mM NaH2PO4, 11.9 mM NaHCO3, 5.6 mM glucose) containing 0.1% gelatin and are sensitized with mouse monoclonal anti-DNP IgE (50 μg/106 cells). Then the cells are washed and resuspended with Tyrode's buffer containing 0.25% BSA. The cells (2×106 cells) are incubated for 5 min at 37°C and challenged with TNP-BSA (2 ng BSA/mL). Quinotolast (0.1, 1, 10, 100 ug/mL) is added to the reaction tube simultaneously with the antigen. Ten minutes later, the reaction is stopped by the addition of EDTA (2.7 mM). pLTs in the cell supernatant sre quantified as immunoreactive leukotriene C4 (iLTC4) with a leukotriene C4/D4/E4[3H] assay system. % Inhibition is calculated in each experiment from the amount of immunoreactive leukotriene C4 (iLTC4)[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

Rats [2]
Rats (8 week-old) are used. To study the presence of tachyphylaxis by Quinotolast, Quinotolast (0.001, 0.01, 0.1, 1,10 and 100 mg/kg) is given i.v. in a large dose 30 min before challenge, and again at a smaller dose simultaneously with the antigen challenge.

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

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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6932 mL 13.4658 mL 26.9317 mL 67.3292 mL
5 mM 0.5386 mL 2.6932 mL 5.3863 mL 13.4658 mL
10 mM 0.2693 mL 1.3466 mL 2.6932 mL 6.7329 mL
15 mM 0.1795 mL 0.8977 mL 1.7954 mL 4.4886 mL
20 mM 0.1347 mL 0.6733 mL 1.3466 mL 3.3665 mL
25 mM 0.1077 mL 0.5386 mL 1.0773 mL 2.6932 mL
30 mM 0.0898 mL 0.4489 mL 0.8977 mL 2.2443 mL
40 mM 0.0673 mL 0.3366 mL 0.6733 mL 1.6832 mL
50 mM 0.0539 mL 0.2693 mL 0.5386 mL 1.3466 mL
60 mM 0.0449 mL 0.2244 mL 0.4489 mL 1.1222 mL
80 mM 0.0337 mL 0.1683 mL 0.3366 mL 0.8416 mL
100 mM 0.0269 mL 0.1347 mL 0.2693 mL 0.6733 mL
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Quinotolast sodium Related Classifications

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:

Quinotolast101193-62-8FR71021FR 71021FR-71021Histamine ReceptorLeukotriene ReceptorProstaglandin ReceptorInhibitorinhibitorinhibit

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