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Purity: ≥98%
VUF10460 is a non-imidazole agonist of the histamine H4 receptor which binds to rat H4 receptor with a pKi of 7.46. The absence of imidazole heterocycle may have contributed to VUF10460's roughly 50-fold selectivity for the rat H4 receptor compared to the H3 receptor, according to radioligand binding studies. Immethridine and methimepip significantly decreased (by 66% and 48%, respectively) the gastric lesions caused by HCl in conscious rats. Moreover, the H4 receptor agonists VUF10460 and VUF8430 significantly increased the lesions caused by HCl, indicating that the selective agonists' activation of histamine H4 receptors exacerbated the ulcerogenic effects of 0.6 N HCl.
| Targets |
H4 ( pKi = 7.46 )
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| Enzyme Assay |
ViF10460 has pKi values of 5.75 and 7.46 for its binding to the rat H3 and H4 receptors, respectively. VUF10460 exhibits a selectivity for the rat H4 receptor that is roughly 50 times greater than that of the H3 receptor. The displacement radioligand binding assay was conducted in a 200 μl total volume of homogenized rat histamine H3 receptor-transfected cells in 50 mM Tris–HCl buffer (pH 7.4 at 25 °C), with or without competing ligands (10− 4 to 10− 11 M). After 60 minutes of incubation at 25 °C, the binding reaction was stopped by quickly filtering through Unifilter GF/C 96-well filterplates (PerkinElmer, USA) that had been pretreated with 0.3% 750 kDa polyethylenimine. This was done three times with ice-cold 50 mM Tris–HCl (pH 7.4 at 4 °C). By using 25 μl of Microscint“O”TM and liquid scintillation counting on the Microbeta Trilux, radioactivity retained on the filter was measured.
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| Cell Assay |
HEK 293 T cells were incubated at 37 °C in a 5% CO2 humidified atmosphere using Dulbeccos modified Eagle medium (DMEM) supplemented with 10% fetal bovine serum (FBS), 50 IU/ml penicillin, and 50 μg/ml streptomycin. Before transfection, about 4 million cells were cultured for an overnight period in a 10-cm dish. To transfect every cell dish, 0.5 ml of serum-free DMEM was used to prepare the transfection mixture. 5 μg of rat histamine H4 or H3 receptor plasmid and 15 μl of 1 mg/ml 25 kDa linear polyethyleneimine (Polyscience, Inc., USA) were added to the mixture, and it was vortexed right away. The mixture was added to the monoloyer cell culture, which was already loaded with 6 ml of fresh cell culture medium, and allowed to incubate for 10 to 15 minutes at room temperature. The cells were scraped off two days after transfection, pelletized by centrifugation, and kept at -20 °C until needed.
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| References |
| Molecular Formula |
C₁₅H₁₉N₅
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| Molecular Weight |
269.34
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| Exact Mass |
269.16
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| Elemental Analysis |
C, 66.89; H, 7.11; N, 26.00
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| CAS # |
1028327-66-3
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| Appearance |
Solid powder
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| SMILES |
CN1CCN(CC1)C2=NC(=NC(=C2)C3=CC=CC=C3)N
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| InChi Key |
NIJGWJIOMPHDBP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H19N5/c1-19-7-9-20(10-8-19)14-11-13(17-15(16)18-14)12-5-3-2-4-6-12/h2-6,11H,7-10H2,1H3,(H2,16,17,18)
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| Chemical Name |
4-(4-methylpiperazin-1-yl)-6-phenylpyrimidin-2-amine
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.28 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (9.28 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (9.28 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7128 mL | 18.5639 mL | 37.1278 mL | |
| 5 mM | 0.7426 mL | 3.7128 mL | 7.4256 mL | |
| 10 mM | 0.3713 mL | 1.8564 mL | 3.7128 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Effects of the selective histamine H4receptor agonists VUF8430 (30mg/kg) and VUF10460 (10mg/kg) on the gastric lesions induced by 0.6N HCl (5ml/kg, Vehicle), in the absence (A) or in the presence (B) of the selective histamine H4receptor antagonist JNJ7777120 (10mg/kg).Eur J Pharmacol.2011 Nov 1;669(1-3):121-7. |
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n the top (A), macroscopic aspects of gastric mucosa from rats treated with Vehicle (saline, 1ml/kg), Vehicle±0.6N HCl (5ml/kg) or immethridine (30mg/kg)+0.6N HCl. On the bottom, effects of immethridine (10mg/kg, B), immethridine (30mg/kg, C) or methimepip (30mg/kg, D) on the gastric ulcerogenic response to 0.6N HCl (Vehicle).Eur J Pharmacol.2011 Nov 1;669(1-3):121-7. |
Effect of the selective histamine H3receptor agonist immethridine (30mg/kg) on the gastric lesions induced by 0.6N HCl (5ml/kg, Vehicle) in the absence or in the presence of the selective histamine H3receptor antagonist A-331440 (30mg/kg, A) or the selective histamine H4receptor antagonist JNJ7777120 (10mg/kg, B).Eur J Pharmacol.2011 Nov 1;669(1-3):121-7. |
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