H4R antagonist 1

H4R antagonist 1 is a highly selective histamine H4 receptor (H4R) antagonist (IC50: 27 nM). H4R antagonist 1 does not show any noticeable binding affinity to other subtypes of histamine receptors, H1R, H2R, and H3R.

产品编号 T11532Cas号 1429375-54-1

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H4R antagonist 1

产品编号 T11532Cas号 1429375-54-1

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规格	价格	库存
2 mg	¥ 3,720	5日内发货
25 mg	¥ 10,600	6-8周
50 mg	¥ 13,800	6-8周
100 mg	¥ 17,500	6-8周

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生物活性

产品描述	H4R antagonist 1 is a highly selective histamine H4 receptor (H4R) antagonist (IC50: 27 nM). H4R antagonist 1 does not show any noticeable binding affinity to other subtypes of histamine receptors, H1R, H2R, and H3R.
靶点活性	H4 receptor (human):27 nM, H4 receptor (mouse):290 nM
体外活性	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 ?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.
体内活性	In the GTPγS functional assay, H4R antagonist 1 shows inhibitory activity against mouse H4R with an IC50 of 0.69 μM.H4R antagonist 1 shows significant antipruritic and anti-inflammatory efficacy in Oxazolone-induced murine model mimicking human atopic dermatitis (AD).

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