Cat. No.: HY-101810

Tazanolast

(Synonyms: TO 188; Tazalest; Tazanol)

Customer Review

Based on 1 Customer Validation

Tazanolast (TO 188) is an orally active selective mast cell stabilizer. Tazanolast prevents the elevation of intracellular calcium concentration, inhibits calcium uptake and Protein kinase C translocation, without directly inhibiting phospholipase C. Tazanolast inhibits ozone-induced airway hyperresponsiveness to Methacholine in guinea pigs, as well as passive cutaneous anaphylaxis, Schultz-Dale reaction, experimental asthma, passive cutaneous anaphylaxis in rats, and increased cutaneous vascular permeability in rats. Tazanolast does not alter airway responsiveness in sham-exposed guinea pigs, cell distribution in bronchoalveolar lavage fluid after ozone exposure, type II-IV allergic reactions, or histamine release from atopic leukocytes. Tazanolast can be used in research related to allergic diseases.

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

Purity: 99.50%
CAS No.: 82989-25-1
Formula: C₁₃H₁₅N₅O₃
Molecular Weight:289.29

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Tazanolast Chemical Structure

CAS No.: 82989-25-1

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(In Japan)

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Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

All Calcium Channel Isoforms :

All PKC Isoforms :

In Vitro

Tazanolast acts as a selective mast cell stabilizer by inhibiting multiple mast cell activation pathways, including histamine release, calcium uptake, protein kinase C translocation, and inositol trisphosphate production, and suppresses the Schultz-Dale reaction in isolated tracheal muscle^[1].
Tazanolast prevents histamine release-inducing intracellular calcium concentration increases in mast cells^[3].

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

In Vivo

Tazanolast (30-300 mg/kg; p.o.; 30 minutes before ozone exposure) significantly inhibits ozone-induced airway hyperresponsiveness in guinea pigs in a dose-dependent manner when administered before ozone exposure, with the 300 mg/kg dose producing the greatest reduction in delta logPC₂₀₀-MCh to 0.09^[1].
Tazanolast (300 mg/kg; p.o.; 30 minutes before sham air exposure) does not affect baseline airway responsiveness or BAL cell distribution in healthy guinea pigs exposed to filtered air^[1].
Tazanolast (10 mg/kg; p.o.) significantly inhibits Ovalbumin (HY-W250978)-induced passive cutaneous anaphylaxis in rats and potently suppresses Substance P- and PGD₂-mediated increases in vascular permeability in rat skin^[2].

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

Animal Model:

Hartley (male, 400 to 600 g, ozone-induced airway hyperresponsiveness)^[1]
Dosage:

30 mg/kg (pre-ozone exposure); 100 mg/kg (pre-ozone exposure); 300 mg/kg (pre-ozone exposure); 300 mg/kg (post-ozone exposure)
Administration:

p.o.; 30 minutes before ozone exposure; p.o.; immediately after ozone exposure
Result:

Inhibited ozone-induced increases in airway responsiveness in a dose-dependent manner, with delta logPC200-MCh values of 0.45 for 30 mg/kg, 0.21 for 100 mg/kg, and 0.09 for 300 mg/kg, all significantly lower than the vehicle group value of 0.65 (p < 0.05, p < 0.01, and p < 0.001, respectively).
Did not produce a delta logPC200-MCh value significantly different from the vehicle group when administered at 300 mg/kg after ozone exposure.
Did not significantly alter BAL cell distribution (neutrophils, macrophages, lymphocytes, eosinophils) at 2 hours after ozone exposure at all tested doses compared to the vehicle group.

Animal Model:

Hartley (male, 400 to 600 g, healthy, sham filtered air exposure)^[1]
Dosage:

300 mg/kg
Administration:

p.o.; 30 minutes before sham air exposure
Result:

Did not alter PC200-MCh compared to baseline values or the vehicle-treated sham exposure group.
Showed no significant differences in BAL cell numbers (macrophages, lymphocytes, eosinophils, neutrophils) between the tazanolast-treated sham group and the vehicle-treated sham group.

Chemical Information

CAS No. 82989-25-1
Appearance Solid
Molecular Weight 289.29
Formula C₁₃H₁₅N₅O₃
Color White to off-white
SMILES

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

TO 188; Tazalest; Tazanol
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 : 100 mg/mL (345.67 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.4567 mL

17.2837 mL

34.5674 mL

5 mM

0.6913 mL

3.4567 mL

6.9135 mL

10 mM

0.3457 mL

1.7284 mL

3.4567 mL

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.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

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In Vivo:

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

Stock Solution Working Solution

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Igarashi A, et al. Tazanolast inhibits ozone-induced airway hyperresponsiveness in guinea pigs. Am J Respir Crit Care Med. 1998 May;157(5 Pt 1):1531-5. [Content Brief]

[2]. Ohtani H, et al. The inhibitory effects of tazanolast on passive cutaneous anaphylaxis (PCA) reaction and increased vascular permeability by various mediators in rats[J]. Japanese Journal of Pharmacology, 1991, 55: 382.

[3]. Csaba G, et al. Prolonged effect of an H1-receptor blocker antihistamine on the histamine content of white blood cells and mast cells. Cell Biochem Funct. 2004 May-Jun;22(3):201-4. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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All Calcium Channel Isoforms

All PKC Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Tazanolast Related Classifications

Cat. No.: HY-101810