2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  3. Histamine Receptor
  4. 4-Methylhistamine

4-Methylhistamine 是一种强效且选择性的组胺 4 受体 (H4R) 激动剂，其 Ki 值为 50 nM。4-Methylhistamine 对 hH4R 的选择性比对其他组胺受体亚型高 100 倍以上。4-Methylhistamine 能强效激活人 H4R (pEC50 值为 7.4)。4-Methylhistamine 可用于癌症、炎症和免疫学方面的研究，如肺癌和皮肤炎症。

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4-Methylhistamine

4-Methylhistamine Chemical Structure

CAS No. : 36507-31-0

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规格 价格 是否有货 数量
1 mg ￥568
3 - 4 周
5 mg   询价  
10 mg   询价  

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Customer Review

Other Forms of 4-Methylhistamine:

4-Methylhistamine 相关抗体

Top Publications Citing Use of Products

查看 Histamine Receptor 亚型特异性产品:

查看所有亚型
H1 Receptor H2 Receptor H3 Receptor H4 Receptor Histamine Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

4-Methylhistamine is a potent and selective agonist of histamine 4 receptor (H4R) with a Ki of 50 nM. 4-Methylhistamine has a >100-fold selectivity for the hH4R over the other histamine receptor subtypes. 4-Methylhistamine can potently activate the hH4R (pEC50 = 7.4). 4-Methylhistamine can be used for the researches of cancer, inflammation and immunology, such as lung cancer and skin inflammation[1][2][3][4].

IC50 & Target[1]

H4 receptor

50 nM (Ki)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Sf9 EC50
12400 nM
Compound: 58
Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
[PMID: 27007611]
体外研究
(In Vitro)

4-Methylhistamine (1-10 μM, 12 h) 可抑制 A549、H157、H460 和 H322 细胞的增殖[4]。
4-Methylhistamine (1 μM, 12 h) 会降低 A549 细胞中 TGF-β1 mRNA 的表达[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

4-Methylhistamine 相关抗体:

Western Blot Analysis[4]

Cell Line: A549, H157, H460 and H322 cells
Concentration: 1 μM
Incubation Time: 12 h
Result: Increased E-cadherin levels and decreased Vimentin levels.
体内研究
(In Vivo)

4-Methylhistamine (30 mg/kg，腹腔注射，在应激前 2 天开始每天两次) 可调节慢性应激对 Balb/c 小鼠 Th1/Th2 细胞因子平衡的影响[2]。
4-Methylhistamine (20-40 mg/kg，腹腔注射，连续 10 天每天一次) 可减轻 Imiquimod (HY-B0180) 诱导的小鼠银屑病样皮肤炎症[3]。
4-Methylhistamine (100 μmol/kg，静脉注射，每两天一次，持续 33 天) 可减小 A549 肿瘤小鼠的平均肿瘤体积并延长其生存期[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Balb/c mice with chronic restraint[2]
Dosage: 30 mg/kg
Administration: Intraperitoneally injection, twice a day before 2 days prior to stress
Result: Increased in the CD4+ T cells as well as in IFN-γ production.
Decreased IL-4 expression.
Upregulated expression of IL-1β, IFN-γ and TNF-α mRNA.
Animal Model: Imiquimod (HY-B0180)-induced psoriasis-like dermatitis mice[3]
Dosage: 20 and 40 mg/kg
Administration: Intraperitoneally injection, once a day for 10 days
Result: Ameliorated the total clinical severity scores.
Attenuated the psoriatic phenotypes, including epidermal hyperplasis, hyperkeratosis and lymphocytes infiltration.
Led to reductions in the levels of Th1 cytokines (TNF-a, IFN-a, and IL-27).
Increased CD4+CD25+FoxP3+ regulatory T (Treg) cells.
Animal Model: A549 tumor mice models[4]
Dosage: 100 μmol/kg
Administration: Intravenously injection, every other day for 33 days
Result: Decreased tumor volume and the proliferation of tumour cells.
Prolonged survival of mice.
Increased the mRNA expression of E-cadherin and decreased Vimentin levels.
分子量

125.17

Formula

C6H11N3
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料

纯度: 90.00%

COA (284 KB)

产品使用指南 (1538 KB)
参考文献

4-Methylhistamine 相关分类

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  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

4-Methylhistamine36507-31-0Histamine ReceptorHistamine 4 receptorH4RA549lung cancerSkin inflammationInhibitorinhibitorinhibit

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