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Quinotolast sodium

Cat No.:V34150 Purity: ≥98%
Quinotolast sodium (concentration range 1-100 μg/mL) inhibits histamine, LTC4 and PGD2 release in a concentration-dependent fashion.
Quinotolast sodium
Quinotolast sodium Chemical Structure CAS No.: 101193-62-8
Product category: New2
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
5mg
10mg
Other Sizes
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Product Description
Quinotolast sodium (concentration range 1-100 μg/mL) inhibits histamine, LTC4 and PGD2 release in a concentration-dependent fashion.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
In dispersed human lung cells, quinotolast inhibits the release of histamine as well as the production of prostaglandin D2 and leukotriene (LT) C4. Quinotolast (100 μg/mL) markedly reduced 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 was largely independent of the preincubation period, and no tachyphylaxis was observed. Quinotolast has a significant inhibitory effect on inflammatory mediators in human dispersed lung cells [1]. Quinotolast also showed strong inhibitory effects on histamine and the peptide leukotrienes released from guinea pig lung fragments or mouse cultured mast cells. Quinotolast concentration-dependently inhibits pLT release from cultured mast cells. The IC50 value of Quinotolast is 0.72 μg/mL[2].
ln Vivo
Quinotolast can effectively suppress type I allergic reactions, including allergic bronchoconstriction and passive cutaneous anaphylaxis (PCA), in rats when administered intravenously and orally. When given intravenously to rats, quinotolast inhibits PCA in a dose-dependent manner. 0.0063 mg/kg of quinolast is the dose needed to suppress the response by 50% (ED50). When taken orally, quinotolast suppresses this reaction. Quinlilast's ED50 value is 0.0081 mg/kg. At a dose of 0.32 mg/kg, Quinotolast almost completely inhibited, but at a dose of 1 mg/kg, its effect was somewhat diminished [2].
References

[1]. Inhibition of histamine and eicosanoid release from dispersed human lung cells in vitro byquinotolast. Jpn J Pharmacol. 1995 Dec;69(4):375-80.

[2]. Effects of quinotolast, a new orally active antiallergic drug, on experimental allergic models. Jpn J Pharmacol. 1993 Sep;63(1):73-81.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C17H11N6NAO3
Molecular Weight
370.297413110733
Exact Mass
371.087
CAS #
101193-62-8
PubChem CID
14600474
Appearance
Light yellow to yellow solid powder
LogP
1.93
Hydrogen Bond Donor Count
1
Hydrogen Bond Acceptor Count
7
Rotatable Bond Count
4
Heavy Atom Count
27
Complexity
726
Defined Atom Stereocenter Count
0
InChi Key
CDPWRMHFRRXOQH-UHFFFAOYSA-M
InChi Code
InChI=1S/C17H12N6O3.Na/c24-15(18-17-19-21-22-20-17)12-10-14(26-11-6-2-1-3-7-11)13-8-4-5-9-23(13)16(12)25;/h1-10H,(H2,18,19,20,21,22,24);/q;+1/p-1
Chemical Name
sodium;4-oxo-1-phenoxy-N-(1,2,3-triaza-4-azanidacyclopenta-2,5-dien-5-yl)quinolizine-3-carboxamide
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~115 mg/mL (~309.71 mM)
Solubility (In Vivo)
Solubility in Formulation 1: 5.75 mg/mL (15.49 mM) 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 57.5 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: 5.75 mg/mL (15.49 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 57.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.7005 mL 13.5026 mL 27.0051 mL
5 mM 0.5401 mL 2.7005 mL 5.4010 mL
10 mM 0.2701 mL 1.3503 mL 2.7005 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.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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.

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