H4R antagonist 1
H4Rantagonist1是一种有效的高选择性组胺H4受体(H4R)拮抗剂，IC50为27nM。H4Rantagonist1对组胺受体的其他亚型H1R，H2R和H3R没有任何明显的结合亲和力。
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包装价格促销价数量
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1mg￥2350.001880.00- +
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5mg￥5825.004660.00- +
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10mg￥9387.007510.00- +
- 货号: ajcx12676
- CAS: 1429375-54-1
- 别名:
- 分子式: C11H11BrN8
- 分子量: 335.16
- 纯度: ＞98%
- 溶解度: Soluble in DMSO
- 储存: Store at -20°C
- 库存: 现货
Background
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].
[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.
