H4R antagonist 1

CAS NO.：1429375-54-1
Empirical Formula: C11H11BrN8
Molecular Weight: 335.16
MDL number: MFCD31813646
Update Date: 2026-04-21 10:31:43

What is H4R antagonist 1?

Description

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

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 (Compound 48) 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[1].

H4R antagonist 1 (Compound 48) shows significant antipruritic and anti-inflammatory efficacy in Oxazolone-induced murine model mimicking human atopic dermatitis (AD)[1]. In the [35S]GTPγS functional assay, H4R antagonist 1 shows inhibitory activity against mouse H4R with an IC50 of 0.69 μM[1].

References

[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.

Properties of H4R antagonist 1

Density	2.13±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	Soluble in DMSO
form	Solid
pka	7.56±0.20(Predicted)
color	Light yellow to yellow

Safety information for H4R antagonist 1

Computed Descriptors for H4R antagonist 1

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