1. GPCR/G Protein
    Immunology/Inflammation
  2. Histamine Receptor
  3. H4R antagonist 1

H4R antagonist 1 

Cat. No.: HY-111501
Handling Instructions

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.

For research use only. We do not sell to patients.

H4R antagonist 1 Chemical Structure

H4R antagonist 1 Chemical Structure

CAS No. : 1429375-54-1

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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].

IC50 & Target[1]

Human H4 Receptor

27 nM (IC50)

Mouse H4 Receptor

290 nM (IC50)

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 (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].

In Vivo

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].

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
Molecular Weight

335.16

Formula

C₁₁H₁₁BrN₈

CAS No.

1429375-54-1

SMILES

CNC(C1)CN1C2=NC3=NC=C(Br)C=C3N4C2=NN=N4

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Room temperature in continental US; may vary elsewhere

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H4R antagonist 1
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HY-111501
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H4R antagonist 1

Cat. No.: HY-111501