JNJ 10191584 maleateSelective H4 receptor antagonist; orally active CAS# 869497-75-6 |
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Quality Control & MSDS
3D structure
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| Cas No. | 869497-75-6 | SDF | Download SDF |
| PubChem ID | 11718163 | Appearance | Powder |
| Formula | C17H19ClN4O5 | M.Wt | 394.81 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | VUF 6002 | ||
| Solubility | Soluble to 50 mM in DMSO | ||
| Chemical Name | (Z)-but-2-enedioic acid;(6-chloro-1H-benzimidazol-2-yl)-(4-methylpiperazin-1-yl)methanone | ||
| SMILES | CN1CCN(CC1)C(=O)C2=NC3=C(N2)C=C(C=C3)Cl.C(=CC(=O)O)C(=O)O | ||
| Standard InChIKey | KOTJFAYEELTYCZ-BTJKTKAUSA-N | ||
| Standard InChI | InChI=1S/C13H15ClN4O.C4H4O4/c1-17-4-6-18(7-5-17)13(19)12-15-10-3-2-9(14)8-11(10)16-12;5-3(6)1-2-4(7)8/h2-3,8H,4-7H2,1H3,(H,15,16);1-2H,(H,5,6)(H,7,8)/b;2-1- | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | 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. |
JNJ 10191584 maleate Dilution Calculator
JNJ 10191584 maleate Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.5329 mL | 12.6643 mL | 25.3286 mL | 50.6573 mL | 63.3216 mL |
| 5 mM | 0.5066 mL | 2.5329 mL | 5.0657 mL | 10.1315 mL | 12.6643 mL |
| 10 mM | 0.2533 mL | 1.2664 mL | 2.5329 mL | 5.0657 mL | 6.3322 mL |
| 50 mM | 0.0507 mL | 0.2533 mL | 0.5066 mL | 1.0131 mL | 1.2664 mL |
| 100 mM | 0.0253 mL | 0.1266 mL | 0.2533 mL | 0.5066 mL | 0.6332 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Inhibitory effects of histamine H4 receptor antagonists on experimental colitis in the rat.[Pubmed:16213481]
Eur J Pharmacol. 2005 Oct 17;522(1-3):130-8.
The histamine H(4) receptor is a G-protein coupled receptor with little homology to the pro-inflammatory histamine H(1) receptor, expressed on cells of the immune system with hematopoietic lineage such as eosinophils and mast cells. The effects of the recently described highly selective histamine H(4) receptor antagonists JNJ 10191584 and JNJ 7777120 have now been investigated on the acute colitis provoked by trinitrobenzene sulphonic acid over 3 days in the rat. Treatment with JNJ 10191584 (10-100 mg/kg p.o., b.i.d.) caused a dose-dependent reduction in macroscopic damage, inhibition of the TNBS-provoked elevation of both colonic myeloperoxidase and tumour necrosis factor-alpha (TNF-alpha), and a reduction in the histologically assessed increase in mucosal and submucosal thickness and neutrophil infiltration. JNJ 7777120 (100 mg/kg p.o., b.i.d.) likewise reduced the macroscopic injury and the increases in colonic myeloperoxidase and TNF-alpha levels. These findings indicate a pro-inflammatory role for the histamine H(4) receptor in this model and suggest a novel pharmacological approach to the treatment of colitis.
Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine h(4) antagonists.[Pubmed:16366610]
J Med Chem. 2005 Dec 29;48(26):8289-98.
Three series of H(4) receptor ligands, derived from indoly-2-yl-(4-methyl-piperazin-1-yl)-methanones, have been synthesized and their structure-activity relationships evaluated for activity at the H(4) receptor in competitive binding and functional assays. In all cases, substitution of small lipophilic groups in the 4 and 5-positions led to increased activity in a [(3)H]histamine radiolabeled ligand competitive binding assay. In vitro metabolism and initial pharmacokinetic studies were performed on selected compounds leading to the identification of indole 8 and benzimidazole 40 as potent H(4) antagonists with the potential for further development. In addition, both 8 and 40 demonstrated efficacy in in vitro mast cell and eosinophil chemotaxis assays.
Synthesis and structure-activity relationships of indole and benzimidazole piperazines as histamine H(4) receptor antagonists.[Pubmed:15454206]
Bioorg Med Chem Lett. 2004 Nov 1;14(21):5251-6.
We describe the structure-activity relationships for a series of ligands structurally related to the recently identified (5-chloro-1H-indol-2-yl)-(4-methyl-piperazin-1-yl)-methanone (1) as histamine H(4) receptor (H(4)R) antagonists. Furthermore, we identified related benzimidazoles as novel lead compounds for the H(4)R. The ligands have been evaluated by radioligand displacement studies and functional assays for their interaction with both the human histamine H(3) and H(4) receptors and exhibit pK(i) values up to 7.5 at the human H(4)R.
