| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| 100mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
Mast cells (histamine release pathway); intracellular calcium signaling. Acitazanolast inhibits histamine release from mast cells by preventing the increase in intracellular calcium concentration, which is a critical event in signal transduction leading to histamine release. As the active metabolite of tazanolast, it mediates the antiallergic effects of the parent compound.
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|---|---|
| ln Vitro |
Acitazanolast demonstrates significant bioactivity as an inhibitor of Plasmodium falciparum (3D7), with potencies varying between 9.4 nM and 6678.0 nM. It shows cytotoxicity against Caco-2 cells at 10 µM after 48 hours. The compound inhibits histamine release from mast cells in vitro, with efficacy demonstrated in various cell-based assays.
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| ln Vivo |
Aerosol administration of WP871 (0.01 and 0.033%) inhibited antigen-induced bronchoconstriction in a dose-dependent fashion in vivo. However, high-dose WP871 (0.1%) inhalation itself produced non-specific bronchoconstriction. Acitazanolast can be used to study type I anaphylaxis caused by IgE antibodies.
|
| Enzyme Assay |
In vitro receptor binding assays for Acitazanolast are not extensively documented. Histamine release assays can be performed using rat mast cells or human basophils. Cells are sensitized with IgE antibodies and stimulated with antigen in the presence of varying concentrations of Acitazanolast. Histamine release into the supernatant is measured using ELISA or fluorometric methods. Intracellular calcium levels can be measured using fluorescent indicators such as Fura-2.
|
| Cell Assay |
Cellular assays for Acitazanolast involve culturing mast cells or basophils. Cells are treated with Acitazanolast at varying concentrations (typically 0.1-100 µM) and stimulated with antigen or calcium ionophore. Histamine release is measured by ELISA. Intracellular calcium concentration is measured using fluorescent calcium indicators. The compound's ability to inhibit histamine release and calcium influx is assessed.
|
| Animal Protocol |
In vivo animal studies for Acitazanolast are conducted in rodent models of allergic airway inflammation or anaphylaxis. The compound is administered orally or via aerosol inhalation. Antigen-induced bronchoconstriction is measured using whole-body plethysmography or airway resistance measurements. Histamine levels in bronchoalveolar lavage fluid are measured. Dosing regimens vary, with aerosol concentrations of 0.01-0.1% being studied.
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| ADME/Pharmacokinetics |
Acitazanolast is soluble in DMSO at 35.71 mg/mL (153.14 mM) with ultrasonic warming to 60°C. It has a molecular weight of 233.19 g/mol and a molecular formula of C9H7N5O3. The compound is typically supplied as a solid with a purity of ≥98%. Detailed pharmacokinetic parameters are not extensively documented.
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| Toxicity/Toxicokinetics |
Acitazanolast is generally considered safe for research use at appropriate concentrations. Comprehensive toxicological data are limited. The compound is intended for research use only and is not approved for human therapeutic applications. Standard laboratory safety precautions should be taken when handling the compound.
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| References |
Kamei C, Mio M, Yoshida T, Saito Y, Toyoda Y, Tsuriya Y. Effect of an active
metabolite of the antiallergic agent tazanolast on histamine release from rat
mast cells. Arzneimittelforschung. 1997 Apr;47(4):390-4. PubMed PMID: 9150859.
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| Additional Infomation |
Acitazanolast compounds belong to the tetrazolium class.
Acitazanolast (MTCC, WP871) is the orally active metabolite of the antiallergic agent tazanolast that inhibits histamine release from mast cells by preventing intracellular calcium increase. It is used in the study of type I anaphylaxis caused by IgE antibodies. The compound is not approved for clinical use and is available for research purposes only. |
| Molecular Formula |
C9H7N5O3
|
|---|---|
| Molecular Weight |
233.18358
|
| Exact Mass |
233.054
|
| CAS # |
114607-46-4
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| PubChem CID |
2006
|
| Appearance |
Light yellow to yellow solid powder
|
| Density |
1.7±0.1 g/cm3
|
| Index of Refraction |
1.719
|
| LogP |
0.29
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
17
|
| Complexity |
311
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1=CC(=CC(=C1)NC(=O)C(=O)O)C2=NNN=N2
|
| InChi Key |
VWQZJJZGISNFOE-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C9H7N5O3/c15-8(9(16)17)10-6-3-1-2-5(4-6)7-11-13-14-12-
|
| Chemical Name |
Oxo-((3-(1H-tetrazol-5-yl)phenyl)amino)acetic acid
|
| Synonyms |
MTCC WP-871 WP 871 WP871.
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| 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 |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~35.71 mg/mL (~153.14 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (8.92 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.2885 mL | 21.4427 mL | 42.8853 mL | |
| 5 mM | 0.8577 mL | 4.2885 mL | 8.5771 mL | |
| 10 mM | 0.4289 mL | 2.1443 mL | 4.2885 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.
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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02176889 | Completed | Dietary Supplement: Lactospore | Healthy | KGK Science Inc. | June 2014 | Phase 1 |
| NCT02783300 | Completed | Drug: GSK3326595 Drug: Pembrolizumab |
Neoplasms | GlaxoSmithKline | August 30, 2016 | Phase 1 |
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