Sarpogrelate hydrochloride

Catalog No.S3706 Synonyms: MCI-9042

For research use only.

Sarpogrelate (MCI-9042) is a selective 5-HT2A antagonist with pKi values of 8.52, 7.43 and 6.57 for 5-HT2A, 5-HT2C and 5-HT2B receptors respectively.

Sarpogrelate hydrochloride Chemical Structure

CAS No. 135159-51-2

Purity & Quality Control

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Biological Activity

Description Sarpogrelate (MCI-9042) is a selective 5-HT2A antagonist with pKi values of 8.52, 7.43 and 6.57 for 5-HT2A, 5-HT2C and 5-HT2B receptors respectively.
Targets
5-HT2A [1]
(Cell-free)
5-HT2C [1]
(Cell-free)
5-HT2B [1]
(Cell-free)
5-HT2B [1]
(Cell-free)
0.2 nM(Kd) 1.1 nM(Kd) 2.1 nM(Ki) 2.1 nM(Kd)
In vitro

Sarpogrelate inhibits thrombus formation, lowers platelet aggregation, inhibits both serotonin-induced coronary artery spasm and contraction in porcine model as well as vascular smooth muscle cell proliferation. Sarpogrelate exibit specificity toward 5-HT2 receptors, since it has lack of significant 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 antagonistic activity[1]. Sarpogrelate specifically inhibited the serotonin-induced cytokine trigger but did not influence platelet-derived growth factor–, endothelin–, or angiotensin II–induced cell proliferation. Sarpogrelate inhibited the serotonin-induced increase in intracellular free ionized calcium concentration, prevented mitogen-activated protein kinase activation, and down-regulated expression of the protooncogenes c-fos and c-jun. Sarpogrelate acted at the G1 phase of the cell cycle[2].

In vivo Sarpogrelate can fully protect albino BALB/c retinas, both structurally and functionally, from light-induced retinopathy[3]. It is used clinically for the treatment of vascular inflammation and atherosclerosis. Sarpogrelate mitigates albuminuria in diabetic nephropathy by hindering glomerular platelet activation. Sarpogrelate ameliorates diabetic nephropathy not only by suppressing macrophage infiltration, but also by anti-inflammatory and anti-fibrotic effects[4].

Protocol (from reference)

Cell Research:[2]
  • Cell lines: Porcine coronary artery smooth muscle cells
  • Concentrations: 1 μmol/L
  • Incubation Time: 96 h
  • Method: Cell number was measured using a Coulter counter 96 hours after treatment in the absence and in the presence of sarpogrelate (1 μmol/L).
Animal Research:[3]
  • Animal Models: BALB/c mice
  • Dosages: 5, 15, 30, 40, or 50 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

DMSO 93 mg/mL
(199.58 mM)
Water 93 mg/mL
(199.58 mM)
Ethanol 30 mg/mL
(64.38 mM)

Chemical Information

Molecular Weight 465.97
Formula

C24H31NO6.HCl

CAS No. 135159-51-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN(C)CC(COC1=CC=CC=C1CCC2=CC(=CC=C2)OC)OC(=O)CCC(=O)O.Cl

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