A 943931 dihydrochloride

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Cat.No. 3753 - A 943931 dihydrochloride | C17H21N5.2HCl | CAS No. 1227675-50-4
Description: Potent and selective H4 antagonist
Chemical Name: 4-((3R)-3-amino-pyrrolidin-1-yl)-6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-d]pyrimidin-2-ylamine
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature

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
Storage Desiccate at RT
Purity ≥98% (HPLC)
CAS Number 1227675-50-4
PubChem ID 56972240
InChI Key ISYUFRNZHUOGLA-CURYUGHLSA-N
Smiles NC1=NC(N4C[C@H](N)CC4)=C2C(C(C=CC=C3)=C3CCC2)=N1.Cl.Cl

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 36.83 100
water 36.83 100

Preparing Stock Solutions

The following data is based on the product molecular weight 368.31. 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.72 mL 13.58 mL 27.15 mL
5 mM 0.54 mL 2.72 mL 5.43 mL
10 mM 0.27 mL 1.36 mL 2.72 mL
50 mM 0.05 mL 0.27 mL 0.54 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

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


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Keywords: A943931 potent selective H4 histamine 4 antagonists histaminergics receptors Histamine H4 Receptors

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Histamine Receptors Scientific Review

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