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Azatadine dimaleate

Name: Azatadine dimaleate
Brand: Selleck Chemicals
SKU: S3186
Rating: 5 (1 reviews)

Synonyms: SCH10649,Azatadine Maleate

Catalog No.S3186 Purity: 99.93%

Azatadine (SCH10649,Azatadine Maleate) is an histamine and cholinergic inhibitor with IC50 of 6.5 nM and 10 nM, respectively.

Azatadine dimaleate Chemical Structure

CAS: 3978-86-7

Selleck's Azatadine dimaleate has been cited by 1 publication

Purity & Quality Control

Batch: Purity: 99.93%

99.93

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Signaling Pathway

Histamine Receptor Signaling Pathway

Choose Selective Histamine Receptor Inhibitors

Biological Activity

Description

Azatadine (SCH10649,Azatadine Maleate) is an histamine and cholinergic inhibitor with IC50 of 6.5 nM and 10 nM, respectively.

Targets

Histamine receptor ^[1]	Cholinergic ^[1]
6.5 nM	10 nM

In vitro
In vitro	95% of Azatadine is biotransformed in Sabouraud dextrose broth within 72 hours treatment with two major metabolites, 7-hydroxyazatadine (25%) and 8-hydroxyazatadine (50%), and two minor metabolites, N-desmethylazatadine and 9-hydroxyazatadine. ^[2]

In Vivo
In vivo	Azatadine delays the onset of dyspnea-induced by aerosolized histamine, acetylcholine and serotonin in the conscious guinea-pig with PD50 of 0.01 mg/kg, 0.739 mg/kg and 0.86 mg/kg. Azatadine protects conscious guinea-pigs against death induced by the intravenous injection of histamine with oral PD50 of 0.009 mg/kg in guinea-pig and 0.22 mg/kg in mice. ^[1] Following a single oral dose of Azatadine (4 mg) in fasted volunteers, a C_max of 3 μg/L has been measured by RIA 4.2 hours after administration. Azatadine is almost completely metabolised by hydroxylation, demethylation and formation of zwitterion isomers by oxidative ring opening. Azatadine (8.8 mg oral) in healthy volunteers results in a Csub>max of 5.9 μg/L at 5.3 hours after treatment and bioavailability of 80%. ^[3] Azatadine (1 mg twice daily for 14 days) is effective in relieving the histamine-mediated symptoms of seasonal allergic rhinitis. ^[4]

References

[4] Katelaris C, et al. Asian Pac J Allergy Immunol, 1990, 8(2), 103-107.

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Chemical Information & Solubility

Molecular Weight	522.55	Formula	C₂₀H₂₂N₂.2C₄H₄O₄
CAS No.	3978-86-7	SDF	Download Azatadine dimaleate SDF
Smiles	CN1CCC(=C2C3=CC=CC=C3CCC4=C2N=CC=C4)CC1.C(=CC(=O)O)C(=O)O.C(=CC(=O)O)C(=O)O
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 105 mg/mL ( (200.93 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 105 mg/mL

Ethanol : Insoluble

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

Preparing Stock Solutions

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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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% DMSO + % + % Tween 80 + % ddH₂O

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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