13585831301
021-59541103 021-60443211
3004967995
13585831301021-59541103 021-604432113004967995
在線訂購 免費訂購熱線：021-59541103 021-60443211
聯系人:高小姐
電話:021-59541103 021-60443211
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詳細地址：上海嘉定區嘉羅公路1661
化學性質：
| 規格 | 1mg 5mg 10mg |
| CAS | 36376-47-3 |
| 別名 | N/A |
| 化學名 | 2-(5-methyl-1H-imidazol-4-yl)ethanamine dihydrochloride |
| 分子式 | C6H11N3.2HCl |
| 分子量 | 198.09 |
| 溶解度 | DMSO: 20 mg/ml,Ethanol: 1 mg/ml,PBS (pH 7.2): 10 mg/ml |
| 儲存條件 | 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 |
產品描述：
4-Methylhistamine dihydrochloride (or 4-methylhistamine) is a selective agonist of H4 receptor with a pEC50 value of 7.4±0.1 (α=1) [1].
In the chemotaxis of mast cells and leukocytes to sites of inflammation, the histamine H4 receptor (H4R) is involved [1].
In transfected cells, 4-methylhistamine bound to hH4R with the highest affinity, compared to the binding to other histamine receptors. The interaction between 4-methylhistamine and hH4R showed a higher selectivity than that between the drug and the H3R and H2R, and H1R by >100-fold and >100,000-fold, respectively. 4-Methylhistamine also had a high affinity for the rat and mouse H4R with Ki values of 73 and 55 nM, respectively, though this affinity was lower than that for hH4R. The agonistic effects of 4-methylhistamine to hH4R were antagonized by JNJ 7777120, a selective H4R antagonist. To the rat and mouse H4R, as a full H4 agonist, 4-methylhistamine showed pEC50 values of 5.6 ± 0.1 and 5.8 ± 0.1, respectively [1].
After being fasted for 18 h, rats were administered intraperitoneally (i.p.) with a single dose of 4-methylhistamine. 2 h later, they were subjected to a intra-articular (i.a.) injection of LPS. In both groups treated with 4-methylhistamine and LPS alone, respectively, the expression of TNF-α and NF-κB was increased, levels of IkB-α were decreased in synovial fluid and whole blood. Further, mRNA levels of IL-1β, TNF-α, and NF-κB were significantly increased. Western blot analysis results also confirmed that the expression of TNF-α, JAK-1, NF-κB and STAT-3 was increased in both 4-methylhistamine and LPS treatment groups. In the inflamed knee tissue of the JNJ 7777120-treated group, these increases were completely inhibited [2].
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原創作者：上海莼試生物技術有限公司
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普票匯款信息
賬 戶 名：上海生物
開 戶 行：中國銀行山東省分行營業部
賬 號：2169 2341 6278
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