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Tazanolast  (Synonyms: TO 188; Tazalest; Tazanol)

Cat. No.: HY-101810 Purity: 99.50%
COA Handling Instructions

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Tazanolast is a selective mast-cell-stabilizing agent, on ozone-induced airway hyperresponsiveness in guinea pigs.

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

Tazanolast Chemical Structure

Tazanolast Chemical Structure

CAS No. : 82989-25-1

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 1098 In-stock
Solution
10 mM * 1 mL in DMSO USD 1098 In-stock
Solid
1 mg USD 345 In-stock
5 mg   Get quote  
10 mg   Get quote  

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Tazanolast Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

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Description

Tazanolast is a selective mast-cell-stabilizing agent, on ozone-induced airway hyperresponsiveness in guinea pigs.

In Vitro

Tazanolast, an orally active mast-cell-stabilizing drug, which has been shown to suppress passive cutaneous anaphylaxis, Schultz-Dale reaction in isolated tracheal muscle, and experimental asthma without antagonistic actions upon histamine- and leukotriene-D4-induced contraction, IgE-mediated or compound 48/80-induced histamine release from mast cells and lung fragments, compound 48/80-induced Ca2+ uptake into mast cells from extracellular medium, compound 48/80-induced translocation of protein kinase C from the cytosol to the membrane fraction of mast cells, and inositol trisphosphate production without directly inhibiting phospholipase C in mast cells[1].

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

Tazanolast Related Antibodies
In Vivo

Tazanolast administered before ozone exposure at doses of 30, 100, or 300 mg/kg inhibits ozone-induced airway hyperresponsiveness in a dose-dependent manner. Tazanolast administered after ozone exposure does not inhibit the airway hyperresponsiveness. Tazanolast does not significantly change the cell distribution of bronchoalveolar lavage (BAL) cells at 2 h after the exposure. Tazanolast significantly inhibits ozone-induced airway hyperresponsiveness in guinea pigs[1].

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

289.29

Formula

C13H15N5O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(OCCCC)C(NC1=CC=CC(C2=NN=NN2)=C1)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 66.67 mg/mL (230.46 mM; Need ultrasonic; 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 3.4567 mL 17.2837 mL 34.5674 mL
5 mM 0.6913 mL 3.4567 mL 6.9135 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • 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: ≥ 2.5 mg/mL (8.64 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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).
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

Purity: 99.50%

COA (245 KB) HNMR (133 KB) RP-HPLC (412 KB) MS (153 KB)

Handling Instructions (2659 KB)
References
Animal Administration
[1]

Pigs[1]
The 10 guinea pigs are also exposed to 2 ppm ozone for 2 h and then are orally administered 300 mg/kg of Tazanolast (T-300 post group). At 2 h after exposure PC200-MCh of each animal is determined. Thereafter, BAL is performed for each animal. On Day 1, preexposure PC200-MCh is determined for 50 guinea pigs. On Day 2, guinea pigs in groups of 10 are orally administered Tazanolast at a dose of 30 mg/kg (T-30 group), 100 mg/kg (T-100 group), or 300 mg/kg (T-300 group), or vehicle alone (vehicle group). After 30 min, the animals are exposed to 2 ppm ozone for 2 h. In addition, the other 10 guinea pigs are also exposed to 2 ppm ozone for 2 h and then are orally administered 300 mg/kg of Tazanolast (T-300 post group). At 2 h after exposure PC200-MCh of each animal is determined. Thereafter, BAL is performed for each animal.

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. 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 3.4567 mL 17.2837 mL 34.5674 mL 86.4185 mL
5 mM 0.6913 mL 3.4567 mL 6.9135 mL 17.2837 mL
10 mM 0.3457 mL 1.7284 mL 3.4567 mL 8.6418 mL
15 mM 0.2304 mL 1.1522 mL 2.3045 mL 5.7612 mL
20 mM 0.1728 mL 0.8642 mL 1.7284 mL 4.3209 mL
25 mM 0.1383 mL 0.6913 mL 1.3827 mL 3.4567 mL
30 mM 0.1152 mL 0.5761 mL 1.1522 mL 2.8806 mL
40 mM 0.0864 mL 0.4321 mL 0.8642 mL 2.1605 mL
50 mM 0.0691 mL 0.3457 mL 0.6913 mL 1.7284 mL
60 mM 0.0576 mL 0.2881 mL 0.5761 mL 1.4403 mL
80 mM 0.0432 mL 0.2160 mL 0.4321 mL 1.0802 mL
100 mM 0.0346 mL 0.1728 mL 0.3457 mL 0.8642 mL
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Tazanolast 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:

Tazanolast82989-25-1TO 188 Tazalest TazanolTO188TO-188OthersInhibitorinhibitorinhibit

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