Sarpogrelate hydrochloride

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Cat.No. 3739 - Sarpogrelate hydrochloride | C24H31NO6.HCl | CAS No. 135159-51-2
Description: Selective 5-HT2A antagonist
Alternative Names: MCI 9042
Chemical Name: Succinic acid mono-(1-dimethylaminomethyl-2-(2-[2-(3-methoxyphenyl)ethyl]phenoxy)ethyl) ester hydrochloride
Purity: ≥99% (HPLC)
Datasheet
Citations
Literature

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.

Select a batch to recalculate based on the batch molecular weight:
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

Safety Datasheet

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


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Keywords: MCI9042 selective 5-HT2A antagonists receptors serotonin MCI 9042 5-HT2A Receptors

Citations for Sarpogrelate hydrochloride

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Literature in this Area

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5-HT Receptors Scientific Review

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Pathways for Sarpogrelate hydrochloride

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