H4R antagonist 1
CAS No. : 1429375-54-1
| Size | Price | Stock |
|---|---|---|
| 5mg | $540 | In-stock |
| 10mg | $870 | In-stock |
| 25mg | $1750 | In-stock |
| 50mg | $2800 | In-stock |
| 100mg | $4500 | In-stock |
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| Cat. No. : | HY-111501 |
| M.Wt: | 335.16 |
| Formula: | C11H11BrN8 |
| Purity: | >98 % |
| Solubility: | DMSO : 20 mg/mL (ultrasonic;warming;heat to 60°C) |
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].
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].
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