A 987306

Cat. No. 3640

A 987306 C18H25N5O [1082954-71-9]

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Chemical Name: (±)-(7aR*,11aR*)-5,6,7a,8,9,10,11,11a-Octahydro-4-(1-piperazinyl)-benzofuran[2,3-h]quinazolin-2-amine

Biological Activity

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).

Technical Data

M.Wt:
327.42
Formula:
C18H25N5O
Solubility:
Soluble to 100 mM in DMSO and to 100 mM in ethanol
Purity:
>98 %
Storage:
Store at -20°C
CAS No:
1082954-71-9

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.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Leurs et al (2009) Molecular and biochemical pharmacology of the histamine H4 receptor. Br.J.Pharmacol. 157 14. PMID: 19413568.

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.

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Keywords: A 987306, supplier, potent, selective, H4, histamine, histaminergic, receptors, antagonists, A987306, Tocris Bioscience, Histamine H4 Receptor Antagonist products

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