H4R antagonist 1
Modify Date: 2025-08-26 18:14:30
H4R antagonist 1 structure
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Common Name | H4R antagonist 1 | ||
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| CAS Number | 1429375-54-1 | Molecular Weight | 335.16 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C11H11BrN8 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of H4R antagonist 1H4R 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]. |
| Name | H4R antagonist 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]. |
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| Related Catalog | |
| Target |
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]. |
| References |
| Molecular Formula | C11H11BrN8 |
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| Molecular Weight | 335.16 |