Thioperamide

Pricing Availability   Qty
说明: H3 antagonist; also H4 inverse agonist
化学名: N-Cyclohexyl-4-(imidazol-4-yl)-1-piperidinecarbothioamide
纯度: ≥99% (HPLC)
说明书
引用文献 (4)
评论
文献 (2)

生物活性 for Thioperamide

Thioperamide is a potent histamine H3 and H4 antagonist/inverse agonist. Ki values are 25 and 27 nM for human recombinant H3 and H4 receptors respectively. Blocks eosinophil shape change (IC50 = 1.4 μM) and chemotaxis (IC50 = 519 nM) induced by histamine. Freely crosses the blood-brain barrier.

技术数据 for Thioperamide

分子量 292.44
公式 C15H24N4S
储存 Store at -20°C
纯度 ≥99% (HPLC)
CAS Number 106243-16-7
PubChem ID 3035905
InChI Key QKDDJDBFONZGBW-UHFFFAOYSA-N
Smiles S=C(NC3CCCCC3)N(CC2)CCC2C1=CNC=N1

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for Thioperamide

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 29.24 100
ethanol 29.24 100

制备储备液 for Thioperamide

以下数据基于产品分子量 292.44。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 3.42 mL 17.1 mL 34.2 mL
5 mM 0.68 mL 3.42 mL 6.84 mL
10 mM 0.34 mL 1.71 mL 3.42 mL
50 mM 0.07 mL 0.34 mL 0.68 mL

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产品说明书 for Thioperamide

分析证书/产品说明书
选择另一批次:

参考文献 for Thioperamide

参考文献是支持产品生物活性的出版物。

Gbahou et al (2006) Compared pharmacology of human H3 and H4 receptors: structure-activity relationships of histamine derivatives. Br.J.Pharmacol. 147 744 PMID: 16432504

Hew et al (1990) Characterisation of histamine H3 receptors in guinea pig ileum with H3 selective ligands. Br.J.Pharmacol. 101 621 PMID: 1963802

Ling et al (2004) Histamine H4 receptor mediates eosinophil chemotaxis with cell shape change and adhesion molecule upregulation. Br.J.Pharmacol. 142 161 PMID: 15131002

Liu et al (2001) Cloning and pharmacological characterization of a fourth histamine receptor (H4) expressed in bone marrow. Mol. Pharmacol. 59 420 PMID: 11179434


If you know of a relevant reference for Thioperamide, please let us know.

按产品操作查看相关产品

查看全部 Histamine H3 Receptor Antagonists

关键词: Thioperamide, Thioperamide supplier, H4, inverse, agonists, H3, antagonists, Receptors, Histamine, histaminergic, 0644, Tocris Bioscience

4 篇 Thioperamide 的引用文献

引用文献是使用了 Tocris 产品的出版物。 Thioperamide 的部分引用包括:

Francis et al (2012) Inhibition of histidine decarboxylase ablates the autocrine tumorigenic effects of histamine in human cholangiocarcinoma. Gut 61 753 PMID: 21873469

Robinson and Dickenson (2001) Activation of the p38 and p42/p44 mitogen-activated protein kinase families by the histamine H(1) receptor in DDT(1)MF-2 cells. Br J Pharmacol 133 1378 PMID: 11498525

Takahashi et al (2002) Targeted disruption of H3 receptors results in changes in brain histamine tone leading to an obese phenotype. J Clin Invest 110 1791 PMID: 12488429

Holden et al (2007) Potentiation of NF-κB-dependent transcription and inflammatory mediator release by histamine in human airway epithelial cells. Saudi J Biol Sci 152 891 PMID: 17891168


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