Sarpogrelate hydrochloride

Catalog No.S3706 Batch:S370602

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Technical Data

Formula

C24H31NO6.HCl
Molecular Weight 465.97 CAS No. 135159-51-2
Solubility (25°C)* In vitro DMSO 93 mg/mL (199.58 mM)
Water 93 mg/mL (199.58 mM)
Ethanol 31 mg/mL (66.52 mM)
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 Assay:[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 Study:[3]
  • Animal Models

    BALB/c mice

  • Dosages

    5, 15, 30, 40, or 50 mg/kg

  • Administration

    i.p.

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.