Azatadine dimaleate

Alias: SCH 10649; azatadine maleate; SCH10649; SCH-10649; Idulamine; Idulian; Lergocil; Optimine; Zadine
Cat No.:V1238 Purity: ≥98%
Azatadine dimaleate (SCH10649; SCH-10649; Idulamine; Idulian; Lergocil; Optimine; Zadine), the dimaleate salt of azatadine,is a potent histamine and cholinergic inhibitor that has beenapproved for treating allergic rhinitis and chronic urticaria.
Azatadine dimaleate Chemical Structure CAS No.: 3978-86-7
Product category: Histamine Receptor
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
10mg
25mg
50mg
100mg
250mg
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1g
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Other Forms of Azatadine dimaleate:

  • Azatadine
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Azatadine dimaleate (SCH10649; SCH-10649; Idulamine; Idulian; Lergocil; Optimine; Zadine), the dimaleate salt of azatadine, is a potent histamine and cholinergic inhibitor that has been approved for treating allergic rhinitis and chronic urticaria. It inhibits cholinergic and histamine receptors with IC50s of 6.5 nM and 10 nM, respectively.

Biological Activity I Assay Protocols (From Reference)
Targets
Histamine receptor ( IC50 = 6.5 nM ); Cholinergic ( IC50 = 10 nM )
ln Vitro

In vitro activity: In Sabouraud dextrose broth, 95% of the azatadine is biotransformed in 72 hours into two major metabolites: 25% and 50% of the metabolites are 7-hydroxyazatadine, and the remaining metabolites are N-desmethylazatadine and 9-hydroxyazatadine.[2]

ln Vivo
Azatadine postpones the onset of dyspnea in conscious guinea pigs caused by aerosolized histamine, acetylcholine, and serotonin with PD50 of 0.01 mg/kg, 0.739 mg/kg and 0.86 mg/kg. Azatadine, with an oral PD50 of 0.009 mg/kg in guinea pigs and 0.22 mg/kg in mice, protects conscious guinea pigs from death caused by an intravenous injection of histamine.[1] After fasting volunteers received a single oral dose of 4 mg of azatadine, RIA measured a Cmax of 3 μg/L 4.2 hours after administration. Azatadine undergoes almost total hydroxylation, demethylation, and oxidative ring opening to form zwitterion isomers. In healthy individuals, 8.8 mg of oral azatadine produces a bioavailability of 80% and a Csub>max of 5.9 μg/L at 5.3 hours post-treatment.[3] The histamine-mediated symptoms of seasonal allergic rhinitis can be effectively relieved with azatadine (1 mg twice daily) for a period of 14 days.[4]
Animal Protocol
0.01 mg/kg, 0.739 mg/kg and 0.86 mg/kg
guinea-pig
References

[1]. Agents Actions . 1974 Oct;4(4):264-70.

[2]. Appl Environ Microbiol . 1996 Sep;62(9):3477-9.

[3]. Clin Pharmacokinet . 1991 Nov;21(5):372-93.

[4]. Asian Pac J Allergy Immunol . 1990 Dec;8(2):103-7.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C28H30N2O8
Molecular Weight
522.55
Exact Mass
522.2
Elemental Analysis
C, 64.36; H, 5.79; N, 5.36; O, 24.49
CAS #
3978-86-7
Related CAS #
Azatadine; 3964-81-6
Appearance
Solid powder
SMILES
CN1CCC(=C2C3=C(C=CC=N3)CCC4=CC=CC=C24)CC1.C(=C\C(=O)O)\C(=O)O.C(=C\C(=O)O)\C(=O)O
InChi Key
SGHXFFAHXTZRQM-SPIKMXEPSA-N
InChi Code
InChI=1S/C20H22N2.2C4H4O4/c1-22-13-10-16(11-14-22)19-18-7-3-2-5-15(18)8-9-17-6-4-12-21-20(17)19;2*5-3(6)1-2-4(7)8/h2-7,12H,8-11,13-14H2,1H3;2*1-2H,(H,5,6)(H,7,8)/b;2*2-1-
Chemical Name
(Z)-but-2-enedioic acid;2-(1-methylpiperidin-4-ylidene)-4-azatricyclo[9.4.0.03,8]pentadeca-1(15),3(8),4,6,11,13-hexaene
Synonyms
SCH 10649; azatadine maleate; SCH10649; SCH-10649; Idulamine; Idulian; Lergocil; Optimine; Zadine
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)
Solubility Data
Solubility (In Vitro)
DMSO: ~105 mg/mL (~200.9 mM)
Water: ~105 mg/mL (~200.9 mM)
Ethanol: <1 mg/mL
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.78 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 25.0 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.

Solubility in Formulation 2: ≥ 2.5 mg/mL (4.78 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (4.78 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


Solubility in Formulation 4: 100 mg/mL (191.37 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.9137 mL 9.5685 mL 19.1369 mL
5 mM 0.3827 mL 1.9137 mL 3.8274 mL
10 mM 0.1914 mL 0.9568 mL 1.9137 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.

Calculator

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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.

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