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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)
250mg电议
500mg电议

产品介绍
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。
Cas No.1429375-54-1
Canonical SMILESCNC(C1)CN1C2=NC3=NC=C(Br)C=C3N4C2=NN=N4
分子式C11H11BrN8
分子量335.16
溶解度Soluble in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.