1429375-54-1
1429375-54-1 structure
- Name: H4R antagonist 1
- Chemical Name: H4R antagonist 1
- CAS Number: 1429375-54-1
- Molecular Formula: C11H11BrN8
- Molecular Weight: 335.16
- Catalog: Signaling Pathways GPCR/G Protein Histamine Receptor
- Create Date: 2019-03-03 11:13:11
- Modify Date: 2024-01-06 13:40:29
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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].
| Name | 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]. |
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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 |
|---|---|
| Molecular Weight | 335.16 |