Potent histamine H4 receptor antagonist (pKi values are 8.24 and 8.47 in human and rat H4 receptors respectively). Displays 162-fold, 620-fold, and > 1600-fold selectivity over human H3, H1 and H2 receptors. Blocks zymosan-induced neutrophil reflux and attenuates thermal hypersensitivity in vivo (ED50 = 42 μmol/kg, ip).
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 327.42. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||3.05 mL||15.27 mL||30.54 mL|
|5 mM||0.61 mL||3.05 mL||6.11 mL|
|10 mM||0.31 mL||1.53 mL||3.05 mL|
|50 mM||0.06 mL||0.31 mL||0.61 mL|
References are publications that support the biological activity of the product.
Liu et al (2008) cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia. J.Med.Chem. 51 7094 PMID: 18983139
Leurs et al (2009) Molecular and biochemical pharmacology of the histamine H4 receptor. Br.J.Pharmacol. 157 14 PMID: 19413568
If you know of a relevant reference for A 987306, please let us know.
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Keywords: A 987306, A 987306 supplier, potent, selective, H4, histamine, histaminergic, receptors, antagonists, A987306, Histamine, Receptors, 3640, Tocris Bioscience
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