Biological Activity
Selective 5-HT2A receptor antagonist (pKi values are 8.52, 7.43 and 6.57 for 5-HT2A, 5-HT2C and 5-HT2B receptors respectively). Displays selectivity over 5-HT1, 5-HT3, 5-HT4 H1, H2, M3, α1-adrenergic, α2-adrenergic and β-adrenergic receptors. Displays cardioprotective activity in vivo.
Compound Libraries
Sarpogrelate hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 465.97 |
| Formula | C24H31NO6.HCl |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 135159-51-2 |
| PubChem ID | 444005 |
| InChI Key | POQBIDFFYCYHOB-UHFFFAOYSA-N |
| Smiles | O=C(CCC(O)=O)OC(CN(C)C)COC1=CC=CC=C1CCC2=CC(OC)=CC=C2.Cl |
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 | 46.6 | 100 | |
| water | 11.65 | 25 |
Preparing Stock Solutions
The following data is based on the product molecular weight 465.97. 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 | 2.15 mL | 10.73 mL | 21.46 mL |
| 5 mM | 0.43 mL | 2.15 mL | 4.29 mL |
| 10 mM | 0.21 mL | 1.07 mL | 2.15 mL |
| 50 mM | 0.04 mL | 0.21 mL | 0.43 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Rashid et al (2003) Identification of the binding sites and selectivity of sarpogrelate, a novel 5-HT2 antagonist, to human 5-HT2A, 5-HT2B and 5-HT2C receptor subtypes by molecular modeling. Life Sci. 73 193 PMID: 12738034
Brasil et al (2002) Blockade of 5-HT(2A) receptors by sarpogrelate protects the heart against myocardial infarction in rats. J.Cardiovasc.Pharmacol.Ther. 7 53 PMID: 12000979
Nishiyama (2009) Acute effects of sarpogrelate, a 5-HT2A receptor antagonist on cytokine production in endotoxin shock model of rats. Eur.J.Pharmacol. 614 122 PMID: 19318092
Keywords: Sarpogrelate hydrochloride, supplier, MCI9042, selective, 5-HT2A, antagonists, receptors, serotonin, MCI, 9042, 5-HT2A, Receptors, 5-HT2A, Receptors, Tocris Bioscience
