Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
パッケージサイズ | 在庫状況 | 単価(税別) |
---|---|---|
25 mg | 約6-8 週間 | ¥ 349,000 |
50 mg | 約6-8 週間 | ¥ 454,500 |
100 mg | 約6-8 週間 | ¥ 574,000 |
説明 | 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. |
ターゲット&IC50 | H4 receptor (human):27 nM, H4 receptor (mouse):290 nM |
In vitro | 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. |
In vivo | 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). |
分子量 | 335.16 |
分子式 | C11H11BrN8 |
CAS No. | 1429375-54-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
You can also refer to dose conversion for different animals. 詳細
bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
H4R antagonist 1 1429375-54-1 GPCR/G Protein Immunology/Inflammation Neuroscience Histamine Receptor H-4R antagonist 1 Inhibitor inhibitor inhibit