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Submit ReviewAn extremely potent histamine H3 antagonist/inverse agonist (pA2=9.93). Also displays partial agonist activity at H4 receptors; induces eosinophil shape change with an EC50 of 3 nM.
Sold with the permission of SCI, Amsterdam
分子量 | 470.65 |
公式 | C14H17ClN4S.2HBr |
储存 | Store at RT |
纯度 | ≥99% (HPLC) |
CAS Number | 145231-35-2 |
PubChem ID | 11213569 |
InChI Key | JIJQPEZAVLJZBO-UHFFFAOYSA-N |
Smiles | Br.Br.ClC1=CC=C(CNC(=N)SCCCC2=CNC=N2)C=C1 |
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
water | 100 |
以下数据基于产品分子量 470.65。 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.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.12 mL | 10.62 mL | 21.25 mL |
5 mM | 0.42 mL | 2.12 mL | 4.25 mL |
10 mM | 0.21 mL | 1.06 mL | 2.12 mL |
50 mM | 0.04 mL | 0.21 mL | 0.42 mL |
参考文献是支持产品生物活性的出版物。
Buckland et al (2003) Histamine induces cytoskeletal changes in human eosinophils via the H4 receptor. Br.J.Pharmacol. 140 1117 PMID: 14530216
Liu et al (2001) Cloning and pharmacological characterization of a fourth histamine receptor (H4) expressed in bone marrow. Mol. Pharmacol. 59 420 PMID: 11179434
Yokoyama et al (1994) Clobenpropit (VUF-9153), a new histamine H3 receptor antagonist, inhibits electrically induced convulsions in mice. Eur.J.Pharmacol. 260 23 PMID: 7957622
Van der Goot et al (1992) Isothiourea analogues of histamine as potent agonists or antagonists of the histamine H3 receptor. Eur.J.Med.Chem. 27 511
If you know of a relevant reference for Clobenpropit dihydrobromide, please let us know.
关键词: Clobenpropit dihydrobromide, Clobenpropit dihydrobromide supplier, H4, partial, agonists, H3, antagonists, inverse, potent, Receptors, Histamine, histaminergic, VUF9153, VUF, 9153, 0752, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Clobenpropit dihydrobromide 的部分引用包括:
Alkan et al (2015) Histidine Decarboxylase Deficiency Prevents Autoimmune Diabetes in NOD Mice. J Immunol 2015 965056 PMID: 26090474
Hedegaard et al (2012) Molecular pharmacology of human NMDA receptors. Neurochem Int 61 601 PMID: 22197913
Femenia et al (2015) Hippocampal-Dependent Antidepressant Action of the H3 Receptor Antagonist Clobenpropit in a Rat Model of Depression. Int J Neuropsychopharmacol 18 PMID: 25762718
Flamand et al (2004) Histamine-induced inhibition of leukotriene biosynthesis in human neutrophils: involvement of the H2 receptor and cAMP. Br J Pharmacol 141 552 PMID: 14744809
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