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Chemical Structure| 618385-01-6 Chemical Structure| 618385-01-6

Structure of Vorapaxar
CAS No.: 618385-01-6

Chemical Structure| 618385-01-6

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Vorapaxar is a thrombin receptor (protease-activated receptor, PAR-1) antagonist.

Synonyms: SCH 530348; MK-5348

4.5 *For Research Use Only !

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Product Details of Vorapaxar

CAS No. :618385-01-6
Formula : C29H33FN2O4
M.W : 492.58
SMILES Code : O=C(O[C@@H]1C)[C@@]2([H])[C@]1([H])[C@@H](/C=C/C3=NC=C(C=C3)C4=CC=CC(F)=C4)[C@]([C@](C5)([H])C2)([H])CC[C@H]5NC(OCC)=O
Synonyms :
SCH 530348; MK-5348
MDL No. :MFCD16038876
InChI Key :ZBGXUVOIWDMMJE-QHNZEKIYSA-N
Pubchem ID :10077130

Safety of Vorapaxar

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Vorapaxar

GPCR

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
EA.hy926 cells 20, 50, 80 µM 1 hour To investigate the effect of Vorapaxar on endothelial cell proliferation under cholesterol stimulation, the results showed that Vorapaxar significantly increased the viability rate of endothelial cells. PMC6522885
THP-1 cells 1 µM To study the effect of Vorapaxar on oxLDL uptake in THP-1 cells, results showed that Vorapaxar reversed thrombin-induced lipid accumulation. PMC8700178

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice ob/ob mice and WD+CCl4 mice Oral 3 mg/kg Once daily for 4 weeks To evaluate the effects of Vorapaxar on the burden of senescent hepatocytes, inflammation, and fibrosis in ob/ob and WD+CCl4 mice. Results showed that Vorapaxar reduced the burden of senescent hepatocytes and improved liver inflammation and fibrosis PMC10524311
C57BL/6 mice ApoE knockout mice Oral 10 mg/kg Diet replaced weekly, duration of 16 weeks To study the effect of Vorapaxar on atherosclerosis in ApoE knockout mice, results showed that Vorapaxar reduced atherosclerotic lesion size and attenuated vascular inflammation. PMC8700178

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00132912 Arterial Obstructive Diseases|... More >>Coronary Disease Less << PHASE2 COMPLETED 2007-01-28 -

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.03mL

0.41mL

0.20mL

10.15mL

2.03mL

1.02mL

20.30mL

4.06mL

2.03mL

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

References

 

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