Home Neuronal Signaling 5-HT Receptor antagonist Sarpogrelate hydrochloride For research use only.

Sarpogrelate hydrochloride

Synonyms: MCI-9042

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

Sarpogrelate hydrochloride Chemical Structure

CAS No. 135159-51-2

Purity & Quality Control

Sarpogrelate hydrochloride Related Products

Signaling Pathway

5-HT Receptor Signaling Pathways

5-HT Receptor Signaling Pathway

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
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].
Cell Research 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).
In Vivo
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].
Animal Research Animal Models BALB/c mice
Dosages 5, 15, 30, 40, or 50 mg/kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 465.97 Formula

C24H31NO6.HCl
CAS No. 135159-51-2 SDF Download Sarpogrelate hydrochloride SDF
Smiles CN(C)CC(COC1=CC=CC=C1CCC2=CC(=CC=C2)OC)OC(=O)CCC(=O)O.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 93 mg/mL ( (199.58 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 93 mg/mL

Ethanol : 31 mg/mL


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