MRE-269(ACT-333679) is a prostaglandin I2 (IP) receptor agonist with a binding affinity for the human IP receptor that is 130-fold greater than that for other human prostanoid receptor.
|Solubility (25°C)||DMSO 84 mg/mL|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
 Shun-Bin Luo, et al. Pharm Biol. Effect of quercetin on the pharmacokinetics of selexipag and its active metabolite in beagles
 Katarina Zmajkovicova, et al. Am J Respir Cell Mol Biol. The Antifibrotic Activity of Prostacyclin Receptor Agonism Is Mediated through Inhibition of YAP/TAZ
 John Gatfield, et al. J Pharmacol Exp Ther. Selexipag Active Metabolite ACT-333679 Displays Strong Anticontractile and Antiremodeling Effects but Low β-Arrestin Recruitment and Desensitization Potential
 N N Orie, et al. Prostaglandins Other Lipid Mediat. Differential actions of the prostacyclin analogues treprostinil and iloprost and the selexipag metabolite, MRE-269 (ACT-333679) in rat small pulmonary arteries and veins
 Keith Morrison, et al. J Pharmacol Exp Ther. Differential effects of Selexipag [corrected] and prostacyclin analogs in rat pulmonary artery
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