AMG 837 is a partial GPR40 agonist with an EC50 value of 13 nM, showcasing 85% of the maximal activity displayed by DHA in standard assay conditions, indicating its high potency and selectivity in vitro. This compound excels as a GPR40 agonist with a notable pharmacokinetic profile, effectively stimulating insulin secretion in a glucose-dependent manner in rodents and demonstrating potent insulin secretion stimulation in MIN6 cells, with efficacy comparable to that observed in aequorin Ca2+-flux assays. Moreover, AMG 837 exhibits a two-fold increase in potency compared to its racemic counterpart on GPR40, with demonstrated activity across rat and mouse GPR40 versions (EC50 = 23 and 13 nM, respectively). It lacks significant activity against PPARα, δ, and γ in cell-based assays, and an analysis against an external panel of 64 receptors revealed negligible activity, except for a weak inhibition (IC50 = 3 μM) on the a2-adrenergic receptor.

AMG 837 sodium salt is a potent GPR40 agonist(EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents. IC50 value: 13 nM (EC50) [1] Target: GPR40 agonist AMG 837 displayed the expected t

LY 303511 hydrochloride is a potent mTOR inhibitor

LY303511, an inactive analogue of LY294002, is a mTOR inhibitor and no inhibition for PI3-K.

Propargite is a pesticide used to kill mites. Propargite induces β-cell necrosis preceded by DNA damage. Propargite induces MIN6 cell death with an IC 50 of 1 μM [1] .

Adenosine-5'-O-(3-thiotriphosphate) (ATPγS), an agonist of the purinergic P2Y11 receptor, prompts inositol phosphate accumulation in CHO-K1 cells harboring the human or canine P2Y11 receptor with EC50 values of 1.2 and 19.3 µM, respectively. At a concentration of 10 µM, ATPγS mitigates Junin virus-induced mRNA boosts pertaining to bone morphogenetic protein 6 (BMP6) and diminishes particle forming units (PFUs) in infected primary rat osteoblasts. Furthermore, when applied at 25 µM, it triggers insulin secretion in MIN6 pancreatic β-cells.

GKA50 stimulates insulin release from mouse islets of Langerhans and MIN6 cells. GKA50 shows significant glucose lowering in high fat fed female rats. GKA50 is a potent glucokinase activator (EC50=33 nM at 5 mM glucose).