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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, CAS 3978-86-7

Pack Size	Availability	Price/USD
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%

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 (insoluble or slightly soluble)

References 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：

GPCR Compound Library Anti-Cancer Drug Library Anti-Cancer Approved Drug Library Drug Repurposing Compound Library Inhibitor Library Anti-Neurodegenerative Disease Compound Library Membrane Protein-targeted Compound Library Histamine & Melatonin Receptor-Targeted Compound Library Anti-Parkinson's Disease Compound Library Target-Focused Phenotypic Screening Library

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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.

Keywords

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

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