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Submit ReviewJNJ 10191584 maleate
Description: Selective H4 antagonist; orally active
Alternative Names: VUF 6002
Chemical Name: 1-[(5-Chloro-1H-benzimidazol-2-yl)carbonyl]-4-methylpiperazine maleate
Purity: ≥99% (HPLC)
Biological Activity for JNJ 10191584 maleate
JNJ 10191584 maleate is a 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 for JNJ 10191584 maleate
JNJ 10191584 maleate is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for JNJ 10191584 maleate
| 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=C\C(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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for JNJ 10191584 maleate
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 19.74 | 50 |
Preparing Stock Solutions for JNJ 10191584 maleate
The following data is based on the product molecular weight 394.81. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 5.07 mL | 25.33 mL | 50.66 mL |
| 2.5 mM | 1.01 mL | 5.07 mL | 10.13 mL |
| 5 mM | 0.51 mL | 2.53 mL | 5.07 mL |
| 25 mM | 0.1 mL | 0.51 mL | 1.01 mL |
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Product Datasheets for JNJ 10191584 maleate
References for JNJ 10191584 maleate
References are publications that support the biological activity of the product.
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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Keywords: JNJ 10191584 maleate, JNJ 10191584 maleate supplier, Selective, H4, receptor, antagonists, orally, active, Receptors, Histamine, histaminergic, JNJ10191584, maleate, VUF6002, silent, antagonist, VUF, 6002, 2441, Tocris Bioscience
3 Citations for JNJ 10191584 maleate
Citations are publications that use Tocris products. Selected citations for JNJ 10191584 maleate include:
Tanaka et al (2016) Histamine H3 receptor antagonist OUP-186 attenuates the proliferation of cultured human breast cancer cell lines Biochemical and Biophysical Research Communication 480 479 PMID: 27773822
Desmadryl et al (2012) Histamine H4 receptor antagonists as potent modulators of mammalian vestibular primary neuron excitability. Br J Pharmacol 167 905 PMID: 22624822
Connelly et al (2009) The histamine H4 receptor is functionally expressed on neurons in the mammalian CNS. Br J Pharmacol 157 55 PMID: 19413571
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Histamine Receptors Scientific Review
Written by Iwan de Esch and Rob Leurs, this review provides a synopsis of the different histamine receptor subtypes and the ligands that act upon them; compounds available from Tocris are listed.