Biological Activity
Potent and selective 5-HT3 receptor antagonist (pIC50 = 7.55). Exhibits 200-fold selectivity for 5-HT3 over 5-HT1A, 5-HT1B and 5-HT2 receptors, and a range of other GPCRs. Blocks the 5-HT-elicited von Bezold-Jarisch reflex in rats and suppresses cisplatin-induced vomiting in ferrets.
Compound Libraries
Dolasetron mesylate is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 420.48 |
| Formula | C19H20N2O3.CH3SO3H |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 115956-13-3 |
| PubChem ID | 60653 |
| InChI Key | PSGRLCOSIXJUAL-VPUTYDRXSA-N |
| Smiles | O=C(O[C@@H]3C[C@H](C5)N(CC(C5C4)=O)[C@@]4([H])C3)C2=CNC1=CC=CC=C12.CS(=O)(O)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 42.05 | 100 | |
| water | 42.05 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 420.48. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.38 mL | 11.89 mL | 23.78 mL |
| 5 mM | 0.48 mL | 2.38 mL | 4.76 mL |
| 10 mM | 0.24 mL | 1.19 mL | 2.38 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.48 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Miller (1993) Pharmacological properties of dolasetron, a potent and selective antagonist at 5-HT3 receptors. Drug Dev. Res. 28 87 PMID:
Keywords: Dolasetron mesylate, supplier, 5-HT3, antagonists, GPCRs, vomiting, potent, selective, antagonism, antiemetic, serotonin, 5-HT3, Receptors, 5-HT3, Receptors, Tocris Bioscience
