Biological Activity
Highly selective histamine H4 receptor silent antagonist; binds with high affinity to the human H4 receptor (Ki = 26 nM). > 540-fold selective over the H3 receptor (Ki = 14.1 μM). Inhibits mast cell and eosinophil chemotaxis in vitro with IC50 values of 138 and 530 nM respectively. Orally active in vivo.
Compound Libraries
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Technical Data
| M. Wt | 394.81 |
| Formula | C13H15ClN4O.C4H4O4 |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 869497-75-6 |
| PubChem ID | 11718163 |
| InChI Key | KOTJFAYEELTYCZ-BTJKTKAUSA-N |
| Smiles | O=C(O)/C=CC(O)=O.ClC(C=C3)=CC2=C3N=C(N2)C(N1CCN(C)CC1)=O |
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 | 19.74 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 394.81. 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.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.53 mL | 12.66 mL | 25.33 mL |
| 5 mM | 0.51 mL | 2.53 mL | 5.07 mL |
| 10 mM | 0.25 mL | 1.27 mL | 2.53 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.51 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Terzioglu et al (2004) Synthesis and structure-activity relationships of indole and benzimidazole piperazines as histamine H4 receptor antagonists. Bioorg.Med.Chem.Lett. 14 5251 PMID: 15454206
Venable et al (2005) Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine H4 antagonists. J.Med.Chem. 48 8289 PMID: 16366610
Varga et al (2005) Inhibitory effects of histamine H4 receptor antagonists on experimental colitis in the rat. Eur.J.Pharmacol. 522 130 PMID: 16213481
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