TUG-891 is a potent and selective agonist of the long chain free fatty acid (LCFA) receptor 4, which demonstrates both potential opportunity and possible challenges to therapeutic agonism. TUG-891 displays similar signaling properties to the LCFA α-linolenic acid at human FFA4, including stimulation of Ca2+ mobilization, β-arrestin-1 and β-arrestin-2 recruitment, and extracellular signal-regulated kinase phosphorylation. Activation of human FFA4 by TUG-891 also resulted in rapid phosphorylation and internalization of the receptor. TUG-891 was also a potent agonist of mouse FFA4, but it showed only limited selectivity over mouse FFA1.
|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||DMSO: ≥ 90 mg/mL|
The pharmacology of TUG-891, a potent and selective agonist of the free fatty acid receptor 4 (FFA4/GPR120), demonstrates both potential opportunity and possible challenges to therapeutic agonism.
Hudson BD, et al. Mol Pharmacol. 2013 Nov;84(5):710-25. PMID: 23979972.
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