DV 7028 hydrochlorideSelective 5-HT2A antagonist; antithrombotic CAS# 133364-62-2 |
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| Cas No. | 133364-62-2 | SDF | Download SDF |
| PubChem ID | 19746041 | Appearance | Powder |
| Formula | C21H26ClFN4O3 | M.Wt | 436.91 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 10 mM in water with gentle warming and to 10 mM in DMSO with gentle warming | ||
| Chemical Name | 3-[2-[4-(4-fluorobenzoyl)piperidin-1-yl]ethyl]-6,7,8,9-tetrahydropyrido[1,2-a][1,3,5]triazine-2,4-dione;hydrochloride | ||
| SMILES | C1CCN2C(=NC(=O)N(C2=O)CCN3CCC(CC3)C(=O)C4=CC=C(C=C4)F)C1.Cl | ||
| Standard InChIKey | MEULLZRAYZSDGF-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C21H25FN4O3.ClH/c22-17-6-4-15(5-7-17)19(27)16-8-11-24(12-9-16)13-14-26-20(28)23-18-3-1-2-10-25(18)21(26)29;/h4-7,16H,1-3,8-14H2;1H | ||
| 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 | Selective 5-HT2A receptor antagonist (Ki = 22 nM for at 5-HT2 receptors). Exhibits no affinity for 5-HT1A, 5-HT1B or 5-HT1D receptors. Inhibits collagen-induced serotonin secretion and platelet aggregation; displays no effect on serotonin uptake by platelets. Shown to inhibit arterial thrombus formation, but not venous thrombosis, in rat models. |
DV 7028 hydrochloride Dilution Calculator
DV 7028 hydrochloride Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.2888 mL | 11.444 mL | 22.888 mL | 45.776 mL | 57.22 mL |
| 5 mM | 0.4578 mL | 2.2888 mL | 4.5776 mL | 9.1552 mL | 11.444 mL |
| 10 mM | 0.2289 mL | 1.1444 mL | 2.2888 mL | 4.5776 mL | 5.722 mL |
| 50 mM | 0.0458 mL | 0.2289 mL | 0.4578 mL | 0.9155 mL | 1.1444 mL |
| 100 mM | 0.0229 mL | 0.1144 mL | 0.2289 mL | 0.4578 mL | 0.5722 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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A potent 5-hydroxytryptamine receptor (5-HT2A) antagonist, DV-7028, delays arterial thrombosis development in rats.[Pubmed:9700856]
Thromb Res. 1998 Jun 15;90(6):259-70.
In our study, we demonstrated that DV-7028: (3-[2-[4-(4-fluorobenzoyl)piperidin-1-yl]ethyl]-6, 7,8,9-tetrahydro-2H-pyrido [1,2,-a]-1,3,5-triazine-2, 4(3H)-dione maleate)--a selective 5-HT2A receptor antagonist, inhibited thrombus formation in the arterial thrombosis model and was completely ineffective in the prevention of venous thrombosis in the rat. In washed platelets prelabelled with 3H-serotonin, DV-7028 inhibited, in a dose-dependent manner, the collagen-induced secretion of serotonin. However, the uptake of serotonin into platelets was not affected by this substance. Administration of DV-7028 also inhibited platelet aggregation in the whole blood and platelet-rich plasma (PRP) induced by collagen, and diminished serotonin-induced aggregation of rat platelets in the presence of a sensitizing but nonaggregating amount of ADP, whereas it did not modify aggregation in PRP when induced by ADP. DV-7028 caused a concentration-dependent, almost parallel shift to the right of the concentration-response to serotonin for its pressor effect in the rat perfused tail artery. The present data demonstrate that DV-7028 exhibits 5-HT2A receptor antagonistic properties in the rat cardiovascular system, exhibits antithrombotic effect in the model of arterial but not venous thrombosis in rats. These results constitute further evidence of the possible importance of serotonin as a mediator of platelet thrombosis in arteries. Moreover, they can provide a useful tool for the prevention of various thrombotic diseases.
Pharmacological profile of a new 5-hydroxytryptamine2 receptor antagonist, DV-7028.[Pubmed:1285670]
Arch Int Pharmacodyn Ther. 1992 Sep-Oct;319:114-28.
The pharmacological profile of DV-7028, a pyrido triazine derivative, showed that it is a potent and selective 5-hydroxytryptamine (5-HT)2 receptor antagonist. DV-7028 bound to 5-HT2 receptors in rat brain membranes with a Ki value of 22 nM and caused shifts to the right of the concentration-contraction curves to 5-HT in rat thoracic aorta and canine femoral arteries, which are attributed to activation of 5-HT2 receptors. The compound was highly active by oral administration (0.1-10 mg/kg) based on blockade of the 5-HT-induced pressor responses in pithed rats. In contrast, DV-7028 had no affinity for 5-HT1A, 5-HT1B and 5-HT1D receptors. The affinity of the compound was 14-26 times greater for the 5-HT2 receptors when compared to 5-HT1C, adrenergic alpha 1, dopamine D2 and histamine H1 receptors. In human platelets, DV-7028 attenuated the aggregation induced by collagen and inhibited the amplifying effect of 5-HT with collagen on platelet aggregation. Furthermore, a 10-day toxicity study revealed that DV-7028 was a safe compound which did not produce lethality at repeated oral doses of 800 mg/kg/day in rats. These results indicate that DV-7028 is a selective and potent 5-HT2 receptor antagonist which is orally active and safe.
