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H4R antagonist 1
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
H4R antagonist 1图片
CAS NO:1429375-54-1
包装与价格:
包装价格(元)
10 mg电议
25 mg电议

产品介绍

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.

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).

Cas No.

1429375-54-1

分子式

C11H11BrN8

分子量

335.16

储存和溶解度

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years