首页 GPCR/G Protein Histamine Receptor H4R antagonist 1
H4R antagonist 1
编号 T11532    
CAS 1429375-54-1     分子式 C11H11BrN8     分子量 335.16
靶点: Human H4 Receptor; Mouse H4 Receptor;
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.
选择批次  
纯度 98.00%
规格 库存 单价 数量
100 mg 待询 待询
500 mg 待询 待询
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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

Human H4 Receptor,27 nM

Mouse H4 Receptor,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).

化学信息

分子量

335.16

分子式

C11H11BrN8

CAS

1429375-54-1

溶解度

( < 1 mg/ml refers to the product slightly soluble or insoluble )

储存条件

store at -80°C

备注

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

配制溶液

1 mg 5 mg 10 mg
1 mM 2.984 ml 14.918 ml 29.836 ml
5 mM 0.597 ml 2.984 ml 5.967 ml
10 mM 0.298 ml 1.492 ml 2.984 ml
50 mM 0.06 ml 0.298 ml 0.597 ml
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