A 987306

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Cat.No. 3640 - A 987306 | C18H25N5O | CAS No. 1082954-71-9
Description: Potent and selective H4 receptor antagonist
Chemical Name: (±)-(7aR*,11aR*)-5,6,7a,8,9,10,11,11a-Octahydro-4-(1-piperazinyl)-benzofuran[2,3-h]quinazolin-2-amine
Purity: ≥98% (HPLC)
Datasheet
Citations

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).

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Technical Data

M. Wt 327.42
Formula C18H25N5O
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1082954-71-9
PubChem ID 25109291
InChI Key DJKJVWJQAVGLHJ-YPMHNXCESA-N
Smiles NC3=NC1=C(C(N4CCNCC4)=N3)CCC2=C1[C@@](CCCC5)([H])[C@@]5([H])O2

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 32.74 100
ethanol 32.74 100

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.

Select a batch to recalculate based on the batch molecular weight:
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

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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


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Keywords: potent selective H4 histamine histaminergic receptors antagonists A987306 Histamine H4 Receptors

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