| CAS NO: | 1429375-54-1 |
| Cas No. | 1429375-54-1 |
| Canonical SMILES | CNC(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 tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation 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. |
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