Sarpogrelate hydrochloride

Catalog No.S3706 Synonyms: MCI-9042

Sarpogrelate hydrochloride Chemical Structure

Molecular Weight(MW): 465.97

Sarpogrelate 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.

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Biological Activity

Description Sarpogrelate 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

Cell Research:[2]
+ Expand
  • 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).
    (Only for Reference)
Animal Research:[3]
+ Expand
  • Animal Models: BALB/c mice
  • Formulation: 0.9% sodium chloride
  • Dosages: 5, 15, 30, 40, or 50 mg/kg
  • Administration: i.p.
    (Only for Reference)

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)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 465.97
Formula

C24H31NO6.HCl

CAS No. 135159-51-2
Storage powder
in solvent
Synonyms MCI-9042

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00147303 Completed Cerebral Infarction Mitsubishi Tanabe Pharma Corporation April 2004 Phase 3
NCT00147303 Completed Cerebral Infarction Mitsubishi Tanabe Pharma Corporation April 2004 Phase 3
NCT00129805 Completed Cerebral Infarction Mitsubishi Tanabe Pharma Corporation January 2001 Phase 3
NCT00129805 Completed Cerebral Infarction Mitsubishi Tanabe Pharma Corporation January 2001 Phase 3

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5-HT Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID