A 943931 dihydrochloride

Cat. No. 3753

A 943931 dihydrochloride C17H21N5.2HCl [1227675-50-4]

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Chemical Name: 4-((3R)-3-amino-pyrrolidin-1-yl)-6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-d]pyrimidin-2-ylamine

Biological Activity

Potent and selective histamine H4 receptor antagonist (pKi values are 7.15 and 8.12 at human and rat receptors respectively). Blocks inflammation in a peritonitis mouse model and displays efficacy in inflammatory pain and neuropathic pain models.

Technical Data

Soluble to 100 mM in water and to 100 mM in DMSO
>98 %
Store at +4°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.

Certificate of Analysis / Safety Data Sheet

Certificate of Analysis: View current batch
Safety Data Sheet: View Safety Data Sheet


Cowart et al (2008) Rotationally constrained 2,4-diamino-5,6-disubstituted pyrimidines: a new class of histamine H4 receptor antagonists with improved druglikeness and in vivo efficacy in pain and inflammation models. J.Med.Chem. 51 6547. PMID: 18817367.

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

Aldi et al (2014) Histamine H4-Receptors Inhibit Mast Cell Renin Release in Ischemia/Reperfusion via PKC{epsilon}-Dependent Aldehyde Dehydrogenase Type-2 Activation. J.Pharmacol.Exp.Ther. 349 508. PMID: 24696042.

If you know of a relevant citation for this product please let us know.

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Keywords: A 943931 dihydrochloride, supplier, A943931, potent, selective, H4, histamine, 4, antagonists, histaminergics, receptors, Histamine H4 Receptor Antagonists

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