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Vorapaxar Sulfate

Cat. No. M6243
Vorapaxar Sulfate Structure
Size Price Availability Quantity
5mg USD 180 In stock
10mg USD 280 In stock
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Quality Control
Biological Activity

Vorapaxar and M20 completely blocked thrombin-stimulated PAR1/β-arrestin association in recombinant cells and abolished thrombin-stimulated calcium influx in washed human platelets and vascular smooth muscle cells. Moreover, vorapaxar and M20 inhibited PAR1 agonist peptide-mediated platelet aggregation in human platelet rich plasma with a steep concentration response relationship. Vorapaxar exhibited high selectivity for inhibition of PAR1 over other platelet GPCRs.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 590.66
Formula C29H35FN2O8S
CAS Number 705260-08-8
Purity 99.95%
Solubility 10 mM in DMSO
Storage at -20°C
References

In vitro pharmacological characterization of vorapaxar, a novel platelet thrombin receptor antagonist.
Hawes BE, et al. Eur J Pharmacol. 2015 Sep 5;762:221-8. PMID: 26022529.

Vorapaxar: a review of its use in the long-term secondary prevention of atherothrombotic events.
Frampton JE, et al. Drugs. 2015 May;75(7):797-808. PMID: 25895464.

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Abmole Inhibitor Catalog 2017




Keywords: Vorapaxar Sulfate supplier, inhibitors

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