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Azatadine dimaleate

Catalog No. T0236   CAS 3978-86-7
Synonyms: SCH10649, Azatadine Maleate

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

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Azatadine dimaleate Chemical Structure
Azatadine dimaleate, CAS 3978-86-7
Pack Size Availability Price/USD Quantity
5 mg In stock $ 30.00
10 mg In stock $ 47.00
25 mg In stock $ 73.00
50 mg In stock $ 97.00
100 mg In stock $ 147.00
200 mg In stock $ 218.00
500 mg In stock $ 369.00
1 mL * 10 mM (in DMSO) In stock $ 51.00
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Purity: 100%
Purity: 99.4%
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Biological Description
Chemical Properties
Storage & Solubility Information
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
Molecular Weight 522.55
Formula C28H30N2O8
CAS No. 3978-86-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: 96 mg/mL (183.7 mM)

DMSO: 97 mg/mL (185.6 mM)

Ethanol: <1 mg/mL

TargetMolReferences and Literature

1. Tozzi S, et al. Agents Actions, 1974, 4(4), 264-270. 2. Zhang D, et al. Appl Environ Microbiol, 1996, 62(9), 3477-3479. 3. Simons FE, et al. Clin Pharmacokinet, 1991, 21(5), 372-393. 4. Katelaris C, et al. Asian Pac J Allergy Immunol, 1990, 8(2), 103-107.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Approved Drug Library Anti-Cancer Drug Library Neuronal Signaling Compound Library Histamine & Melatonin Receptor-Targeted Compound Library Anti-Obesity Compound Library ReFRAME Related Library Bioactive Compound Library Anti-Parkinson's Disease Compound Library Approved Drug Library GPCR Compound Library

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Keywords

Azatadine dimaleate 3978-86-7 GPCR/G Protein Immunology/Inflammation Neuroscience AChR Histamine Receptor 5-HT Receptor SCH-10649 inhibit Azatadine SCH 10649 Inhibitor SCH10649 Azatadine Maleate Azatadine Dimaleate inhibitor

 

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