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.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||10 mM in DMSO|
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.
VH-298 is a potent VHL inhibitor that stabilizes HIF-α and elicits a hypoxic response via a different mechanism, with a Kd value of 80 to 90 nM.
6-Methylcoumarin belongs to the class of organic compounds known as coumarins and derivatives.
BTTAA is a Cu(I)-stabilizing ligand, whch performs potently with ubiquitin Glu18AzF.
Ezutromid (also known as BMN-195 and SMT C1100) is a first orally bioavailable utrophin's translation modulator with EC50 of 0.4 uM.
GNE-495 is a potent and selective MAP4K4 inhibitor with an IC50 of 3.7 nM.
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