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Bamirastine

Catalog No. T13566 CAS 215529-47-8

Synonyms: TAK-427

Bamirastine inhibits ligand binding to recombinant human histamine H1 receptor (rhH1R) with an IC50 value of 17.3 nM.Bamirastine has an inhibitory effect on allergic skin inflammation.

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Bamirastine, CAS 215529-47-8

Pack Size	Availability	Price/USD	Quantity
1 mg	In stock	$ 700.00
5 mg	In stock	$ 1,800.00

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Purity: 96.68%

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Description	Bamirastine inhibits ligand binding to recombinant human histamine H1 receptor (rhH1R) with an IC50 value of 17.3 nM.Bamirastine has an inhibitory effect on allergic skin inflammation.
Targets&IC50	H1 receptor (recombinant human):17.3 nM
In vitro	In a concentration-dependent manner, Bamirastine (TAK-427) reduces the specific binding of [3H] pyrilamine to recombinant human H1 receptors (rhH1R) with an IC50 value of 17.3 nM. The calculated Ki value for this interaction is 7.35 nM. Notably, the affinity of Bamirastine is determined to be as high as that of azelastine, 2 times lower than that of Epinastine, 8 times lower than that of ketotifen, and 3 times higher than that of Terfenadine[1].
In vivo	Bamirastine (TAK-427) exhibits inhibition of histamine-induced skin reactions in guinea pigs and mice, with ID50 values of 0.884 and 0.450 mg/kg, p.o., respectively. Notably, significant inhibition persists 24 hours after dosing in guinea pigs even at a dose of 10 mg/kg. However, even at a high dose of 300 mg/kg, Bamirastine does not affect pentobarbital-induced sleeping time in mice. Furthermore, Bamirastine significantly inhibits passive cutaneous anaphylaxis (PCA) in both mice and guinea pigs. Additionally, it inhibits antigen-induced immediate skin reactions (ISRs) in guinea pigs[1].

Synonyms	TAK-427
Molecular Weight	527.66
Formula	C31H37N5O3
CAS No.	215529-47-8

Storage

store at low temperature

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

References and Literature

1. Fukuda S, et al. Characteristics of the antihistamine effect of TAK-427, a novel imidazopyridazine derivative. Inflamm Res. 2003 May;52(5):206-14.

Related compound libraries

This product is contained In the following compound libraries：

GPCR Compound Library

Related Products

Related compounds with same targets

Mepyramine maleate (R)-(-)-α-Methylhistamine dihydrobromide Bepotastine Besilate Escitalopram Nizatidine Daurinoline PF-03654746 Tosylate PF-03654764

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Keywords

Bamirastine 215529-47-8 GPCR/G Protein Immunology/Inflammation Neuroscience Histamine Receptor TAK427 TAK-427 TAK 427 inhibitor inhibit

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