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Azatadine dimaleate

Azatadine dimaleate
Azatadine dimaleate (SCH10649) is an inhibitor for histamine(IC50=6.5 nM) and cholinergic(IC50=10 nM).
Catalog No. T0236Cas No. 3978-86-7
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Azatadine dimaleate

Catalog No. T0236Cas No. 3978-86-7

Azatadine dimaleate (SCH10649) is an inhibitor for histamine(IC50=6.5 nM) and cholinergic(IC50=10 nM).
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Pack SizePriceAvailabilityQuantity
25 mg$39In Stock
50 mg$60In Stock
100 mg$98In Stock
200 mg$143In Stock
1 mL x 10 mM (in DMSO)$29In Stock
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Product Introduction

Bioactivity
Description
Azatadine dimaleate (SCH10649) is an inhibitor for histamine(IC50=6.5 nM) and cholinergic(IC50=10 nM).
Targets&IC50
Histamine receptor:6.5 nM, Cholinergic:10 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]
AliasSCH10649, Azatadine Maleate
Chemical Properties
Molecular Weight522.55
FormulaC28H30N2O8
Cas No.3978-86-7
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
H2O: 96 mg/mL (183.7 mM)
DMSO: 97 mg/mL (185.6 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
Solution Preparation Table
H2O/DMSO
1mg5mg10mg50mg
1 mM1.9137 mL9.5685 mL19.1369 mL95.6846 mL
5 mM0.3827 mL1.9137 mL3.8274 mL19.1369 mL
10 mM0.1914 mL0.9568 mL1.9137 mL9.5685 mL
20 mM0.0957 mL0.4784 mL0.9568 mL4.7842 mL
50 mM0.0383 mL0.1914 mL0.3827 mL1.9137 mL
100 mM0.0191 mL0.0957 mL0.1914 mL0.9568 mL

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