JNJ 10191584 maleate

Name: JNJ 10191584 maleate
Brand: Tocris Bioscience
SKU: 2441

Tocris Bioscience, part of Bio-Techne | Catalog # 2441

Citations (5)

COA / SDS

Selective H4 antagonist; orally active

Key Product Details

Description:	Selective H₄ antagonist; orally active
Alternative Names:	VUF 6002
Chemical Name:	1-[(5-Chloro-1H-benzimidazol-2-yl)carbonyl]-4-methylpiperazine maleate
Purity:	≥98% (HPLC)
Molecular Weight:	394.81

View Full Technical Details for JNJ 10191584 maleate

Technical Data
Citations

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 (K_i = 26 nM). > 540-fold selective over the H₃ receptor (K_i = 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	≥98% (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 for JNJ 10191584 maleate

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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	0.10 mL	0.51 mL	1.01 mL

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References for JNJ 10191584 maleate

References are publications that support the biological activity of the product.

Venable Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine H₄ antagonists. J.Med.Chem. 2005 PMID: 16366610
Varga Inhibitory effects of histamine H₄ receptor antagonists on experimental colitis in the rat. Eur.J.Pharmacol. 2005 PMID: 16213481
Terzioglu Synthesis and structure-activity relationships of indole and benzimidazole piperazines as histamine H₄ receptor antagonists. Bioorg.Med.Chem.Lett. 2004 PMID: 15454206