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Chemical Structure| 135159-51-2 Chemical Structure| 135159-51-2

Structure of Sarpogrelate HCl
CAS No.: 135159-51-2

Chemical Structure| 135159-51-2

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Sarpogrelate HCl is an antagonist of both 5HT2A and 5-HT2B receptors, which can block serotonin-induced platelet aggregation and treat diabetes mellitus, Buerger's disease, Raynaud's disease, coronary artery disease, angina pectoris and atherosclerosis.

Synonyms: MCI-9042; Sarpogrelate (hydrochloride); Sarpogrelate hydrochloride

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Product Details of Sarpogrelate HCl

CAS No. :135159-51-2
Formula : C24H32ClNO6
M.W : 465.97
SMILES Code : O=C(OC(COC1=CC=CC=C1CCC2=CC=CC(OC)=C2)CN(C)C)CCC(O)=O.[H]Cl
Synonyms :
MCI-9042; Sarpogrelate (hydrochloride); Sarpogrelate hydrochloride
MDL No. :MFCD00887582
InChI Key :POQBIDFFYCYHOB-UHFFFAOYSA-N
Pubchem ID :444005

Safety of Sarpogrelate HCl

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H302-H319-H332-H372-H400
Precautionary Statements:P260-P264-P270-P273-P280-P301+P312+P330-P304+P312-P305+P351+P338-P314-P337+P313-P391-P501
Class:9
UN#:3077
Packing Group:

Related Pathways of Sarpogrelate HCl

GPCR

Isoform Comparison

Biological Activity

Target
  • 5-HT2

    5-HT2C, Kd:1.1 nM

    5-HT2A, Kd:2.1 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
MDCK-II-BCRP cells 0.2, 1, 10 µM 1 hour Evaluate the inhibitory effects of Sarpogrelate and M-1 on BCRP-mediated prazosin transport, showing no significant inhibition Drug Des Devel Ther. 2016 Sep 14;10:2959-2972
MDCK-II-P-gp cells 0.2, 1, 10 µM 1 hour Evaluate the inhibitory effects of Sarpogrelate and M-1 on P-gp-mediated loperamide transport, showing <10% inhibition Drug Des Devel Ther. 2016 Sep 14;10:2959-2972
Cardiomyocytes 1 µM 48 hours Suppressed cardiomyocyte hypertrophy induced by PE, Ang II, and ET-1 Pharmaceuticals (Basel). 2021 Dec 5;14(12):1268

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Albino BALBc/J mice Light-induced retinopathy model Intraperitoneal injection 25 mg/kg Single dose, lasting 1 hour To investigate the neuroprotective effects and mechanisms of Sarpogrelate in a light-induced retinopathy model. Results showed that Sarpogrelate exerts neuroprotection through transient activation of the MAPK/ERK pathway and sustained activation of CREB, leading to transcription of anti-apoptotic genes Bcl2, Xiap, and Ucp3. Invest Ophthalmol Vis Sci. 2018 Jan 1;59(1):462-471
C57BL/6J male mice Transverse aortic constriction (TAC) surgery-induced heart failure model Oral 5 mg/kg Once daily for 8 weeks Suppressed TAC-induced cardiac hypertrophy and systolic dysfunction Pharmaceuticals (Basel). 2021 Dec 5;14(12):1268
New Zealand white rabbits High cholesterol diet-induced atherosclerosis model Oral 5 mg/kg/day Once daily for 90 days To investigate the effects of SP on high cholesterol diet-induced atherosclerosis. Results showed that SP reduced plasma cholesterol and triglyceride levels, decreased oxidative stress and blood viscosity, and inhibited the formation of atherosclerotic plaques. J Cell Mol Med. 2012 Oct;16(10):2394-400
BALB/c mice Light-induced retinopathy model Intraperitoneal injection 5, 15, 30, 40, 50 mg/kg 48, 24, and 0 hours before and 24 and 48 hours after exposure To evaluate the protective effect of sarpogrelate on light-induced retinopathy. Results showed that a 50 mg/kg dose completely protected retinal morphology and function. Invest Ophthalmol Vis Sci. 2015 Jul;56(8):4560-9

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00147303 Cerebral Infarction PHASE3 COMPLETED 2025-01-05 -

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.15mL

0.43mL

0.21mL

10.73mL

2.15mL

1.07mL

21.46mL

4.29mL

2.15mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
The prepared working fluid is recommended to be prepared now and used up as soon as possible in a short period of time. The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1

References

 

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