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Submit ReviewDV 7028 hydrochloride
Description: Selective 5-HT2A antagonist; antithrombotic
Chemical Name: 3-[2-[4-(4-Fluorobenzoyl)-1-piperidinyl]ethyl]-6,7,8,9-tetrahydro-2H-pyrido[1,2-a]-1,3,5-triazine-2,4(3H)-dione hydrochloride
Purity: ≥99% (HPLC)
Biological Activity
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.
Technical Data
| M. Wt | 436.91 |
| Formula | C21H25FN4O3.HCl |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 133364-62-2 |
| PubChem ID | 19746041 |
| InChI Key | MEULLZRAYZSDGF-UHFFFAOYSA-N |
| Smiles | O=C(C4=CC=C(F)C=C4)C(CC3)CCN3CCN2C(N1CCCCC1=NC2=O)=O.Cl |
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 | |||
| water | 4.37 | 10 with gentle warming | |
| DMSO | 4.37 | 10 with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 436.91. 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 |
|---|---|---|---|
| 0.1 mM | 22.89 mL | 114.44 mL | 228.88 mL |
| 0.5 mM | 4.58 mL | 22.89 mL | 45.78 mL |
| 1 mM | 2.29 mL | 11.44 mL | 22.89 mL |
| 5 mM | 0.46 mL | 2.29 mL | 4.58 mL |
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References
References are publications that support the biological activity of the product.
Pawlak et al (1998) A potent 5-hydroxytryptamine receptor (5-HT2A) antagonist, DV-7028, delays arterial thrombosis development in rats. Thromb.Res. 90 259 PMID: 9700856
Shibano et al (1992) Pharmacological profile of a new 5-hydroxytryptamine 2 receptor antagonist, DV-7028. Arch.Int.Pharmacodyn.Ther. 319 114 PMID: 1285670
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