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H4R antagonist 1

Catalog No. T11532 CAS 1429375-54-1

H4R antagonist 1 is a highly selective histamine H4 receptor (H4R) antagonist (IC50: 27 nM). H4R antagonist 1 does not show any noticeable binding affinity to other subtypes of histamine receptors, H1R, H2R, and H3R.

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H4R antagonist 1, CAS 1429375-54-1

Pack Size	Availability	Price/USD
25 mg	6-8 weeks	$ 1,520.00
50 mg	6-8 weeks	$ 1,980.00
100 mg	6-8 weeks	$ 2,500.00

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Biological Description

Chemical Properties

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Description	H4R antagonist 1 is a highly selective histamine H4 receptor (H4R) antagonist (IC50: 27 nM). H4R antagonist 1 does not show any noticeable binding affinity to other subtypes of histamine receptors, H1R, H2R, and H3R.
Targets&IC50	H4 receptor (human):27 nM, H4 receptor (mouse):290 nM
In vitro	The competitive binding assay against a wider panel of GPCR, ion channel, and transporters at the concentration of 10 μM reveals that H4R antagonist 1 ?is highly selective for H4R.?The inhibitory activity of H4R antagonist 1 against mouse H4R (IC50=0.29 μM) is about 10 times weaker than that for human H4R.
In vivo	In the GTPγS functional assay, H4R antagonist 1 shows inhibitory activity against mouse H4R with an IC50 of 0.69 μM.H4R antagonist 1 shows significant antipruritic and anti-inflammatory efficacy in Oxazolone-induced murine model mimicking human atopic dermatitis (AD).

Molecular Weight	335.16
Formula	C11H11BrN8
CAS No.	1429375-54-1

Storage

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

References and Literature

1. Ko K, et al. Discovery of a Novel Highly Selective Histamine H4 Receptor Antagonist for the Treatment of Atopic Dermatitis. J Med Chem. 2018 Apr 12;61(7):2949-2961.

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Keywords

H4R antagonist 1 1429375-54-1 GPCR/G Protein Immunology/Inflammation Neuroscience Histamine Receptor H-4R antagonist 1 inhibitor inhibit

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