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Merck
CN

S5451

Sarpogrelate hydrochloride

≥98% (HPLC)

Synonym(s):

Anplag, Butanedioic acid 1-[2-(dimethylamino)-1-[[2-[2-(3-methoxyphenyl)ethyl]phenoxy]methyl]ethyl] ester hydrochloride, MCI 9042, Succinic acid mono-(1-dimethylaminomethyl-2-(2-[2-(3-methoxyphenyl)et hyl]phenoxy)ethyl) ester hydrochloride

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About This Item

Empirical Formula (Hill Notation):
C24H31NO6.HCl
CAS Number:
135159-51-2
Molecular Weight:
465.97
NACRES:
NA.77
PubChem Substance ID:
329824454
UNSPSC Code:
12352200
MDL number:
MFCD00887582

Key Documents

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InChI key

POQBIDFFYCYHOB-UHFFFAOYSA-N

SMILES string

Cl.COc1cccc(CCc2ccccc2OCC(CN(C)C)OC(=O)CCC(O)=O)c1

InChI

1S/C24H31NO6.ClH/c1-25(2)16-21(31-24(28)14-13-23(26)27)17-30-22-10-5-4-8-19(22)12-11-18-7-6-9-20(15-18)29-3;/h4-10,15,21H,11-14,16-17H2,1-3H3,(H,26,27);1H

assay

≥98% (HPLC)

form

solid

storage condition

desiccated

solubility

deionized water: ≥5 mg/mL

storage temp.

room temp

Quality Level

100

General description

Sarpogrelate hydrochloride binds to the serotonin receptor (5-hydroxytryptamine, 5-HT2A). Its binding to 5-HT2A receptor inhibits thrombus formation and reduces platelet aggregation. Sarpogrelate hydrochloride has been used as an anti-atherosclerotic agent. It improves the endothelial function and may be useful for treating peripheral arterial disease. Use of sarpogrelate hydrochloride as 5-HT2A antagonist reduces urinary albumin levels in diabetic nephropathy.

Biochem/physiol Actions

Sarapogrelate hydrochloride is a potent and selective 5-HT2A receptor antagonist.
Sarapogrelate hydrochloride is a potent and selective 5-HT2A receptor antagonist. It exhibits analgesic effects in numerous animal studies.

pictograms

Exclamation markEnvironment
GHS07,GHS09

signalword

Warning

hcodes

H302,H410

Hazard Classifications

Acute Tox. 4 Oral - Aquatic Acute 1 - Aquatic Chronic 1

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Regulatory Information

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Certificates of Analysis (COA)

Lot/Batch Number
0000493138
0000493138
0000484238
0000484238
0000162963

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Daniel Duerschmied et al.
PloS one, 7(2), e32656-e32656 (2012-03-03)
Increased residual platelet reactivity remains a burden for coronary artery disease (CAD) patients who received a coronary stent and do not respond sufficiently to treatment with acetylsalicylic acid and clopidogrel. We hypothesized that serotonin antagonism reduces high on-treatment platelet reactivity.
Sarpogrelate hydrochloride, a selective 5-HT2A antagonist, improves vascular function in patients with peripheral arterial disease
Miyazaki M, et al.
Journal of Cardiovascular Pharmacology, 49(4), 221-227 (2007)
Shaoxin Ma et al.
Journal of diabetes investigation, 7(6), 833-844 (2016-11-03)
Our previous study found that dexamethasone-induced insulin resistance (IR) was involved in 5-hydroxytryptamine (5-HT) synthesis and 5-hydroxytryptamine 2 receptor (5-HT Male rats were exposed to dexamethasone for 10 days, then treated with or without a 5-HT Dexamethasone-induced whole-body IR, with
Yohei Kawano et al.
Biological & pharmaceutical bulletin, 44(2), 238-244 (2021-02-02)
Mirtazapine (MTZ) is a noradrenergic and specific serotonergic antidepressant. MTZ is reportedly associated with an increased risk of bleeding. However, the underlying mechanism remains unclear. In this study, we investigated the antiplatelet effect of MTZ in mice via light transmission
Identification of a key amino acid of the human 5-HT2B serotonin receptor important for sarpogrelate binding
Muntasir HA, et al.
Journal of Pharmacological Sciences, 104(3), 274-277 (2007)
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