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Azatadine dimaleate

Name: Azatadine dimaleate
Brand: TargetMol
SKU: T0236
Price: 36 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T0236Cas No. 3978-86-7

Alias SCH10649, Azatadine Maleate

Azatadine dimaleate (SCH10649) is an inhibitor for histamine（IC50=6.5 nM） and cholinergic（IC50=10 nM）.

Azatadine dimaleate

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Purity: 99.7%

Catalog No. T0236Alias SCH10649, Azatadine MaleateCas No. 3978-86-7

Azatadine dimaleate (SCH10649) is an inhibitor for histamine（IC50=6.5 nM） and cholinergic（IC50=10 nM）.

Pack Size	Price	USA Warehouse	Global Warehouse
50 mg	$36	In Stock	In Stock
100 mg	$59	In Stock	In Stock
200 mg	$86	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:99.7%

Appearance:Solid

Color:White

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COA HNMR HPLC LCMS

Product Introduction

Bioactivity

Description	Azatadine dimaleate (SCH10649) is an inhibitor for histamine（IC50=6.5 nM） and cholinergic（IC50=10 nM）.
Targets&IC50	Cholinergic:10 nM, Histamine receptor:6.5 nM
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	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 Cmax 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]
Synonyms	SCH10649, Azatadine Maleate

Chemical Properties

Molecular Weight	522.55
Formula	C₂₈H₃₀N₂O₈
Cas No.	3978-86-7
Smiles	OC(=O)\C=C/C(O)=O.OC(=O)\C=C/C(O)=O.CN1CC\C(CC1)=C1\c2ccccc2CCc2cccnc12
Relative Density.	no data available

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

H2O: 96 mg/mL (183.71 mM), Sonication is recommended.

DMSO: 97 mg/mL (185.63 mM), Sonication is recommended.

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (6.32 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

H2O/DMSO

	1mg	5mg	10mg	50mg
1 mM	1.9137 mL	9.5685 mL	19.1369 mL	95.6846 mL
5 mM	0.3827 mL	1.9137 mL	3.8274 mL	19.1369 mL
10 mM	0.1914 mL	0.9568 mL	1.9137 mL	9.5685 mL
20 mM	0.0957 mL	0.4784 mL	0.9568 mL	4.7842 mL
50 mM	0.0383 mL	0.1914 mL	0.3827 mL	1.9137 mL
100 mM	0.0191 mL	0.0957 mL	0.1914 mL	0.9568 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc