GSK137647A is a selective FFA4 agonist for human, Mouse and Rat FFA4 with pEC50 values of 6.3, 6.2 and 6.1, respectively. GSK137647A is shown to provide at least 100-fold selectivity against the panel which included 41 G-protein-coupled receptors. Under high glucose conditions (25 mM), GSK137647A produces a concentration-dependent increase in glucose stimulated insulin secretion.
|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 30 mg/mL|
Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120).
Sparks SM, et al. Bioorg Med Chem Lett. 2014 Jul 15;24(14):3100-3. PMID: 24881566.
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