JNJ 10191584 maleate

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Cat.No. 2441 - JNJ 10191584 maleate | C13H15ClN4O.C4H4O4 | CAS No. 869497-75-6
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)
Datasheet
Citations (3)
Reviews
Literature (3)

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.

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=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

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 the degree 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
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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References

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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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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