R&D Systems Inc. Tocris Bioscience Boston Biochem

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

M.Wt:
368.31
Formula:
C17H21N5.2HCl
Solubility:
Soluble to 100 mM in water and to 100 mM in DMSO
Purity:
>98 %
Storage:
Store at +4°C
CAS No:
1227675-50-4

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.

Certificate of Analysis / Safety Data Sheet

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

References

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.. 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

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