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A DPP-4 inhibitor (IC50 0.01 UM) selective for DPP-4 over DPP-8 DPP-9 and FAP- a (IC50s 277.28 233.72 418.43 UM respectively) inhibits DPP-4 activity in isolated human plasma (IC50 11.5 nM) scavenges methylglyoxal in vitro and inhibits AGE formation between BSA and methylglyoxal and cross-linking of AGE-BSA with rat tail tendon collagen (IC50s 1.15 11.69 and 1.39 mM respectively) reduces the levels of circulating AGE and red blood cell IgG content in db/db diabetic mice at 100 mg/kg decreases blood glucose and HbA1c levels and reduces pancreaticBcell damage in a mouse model of STZ- and high-fat diet-induced diabetes induces cytotoxicity in SW1736 and TPC-1 cells
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PD-118057 is an activator of the hERG channel that does not induce hERG blockade. It operates by activating the hERG channel, thereby helping to suppress changes in membrane excitability. Studies have shown that it specifically enhances hERG current and inhibits action potential duration in guinea pig ventricular muscle and cardiomyocytes. Additionally, it can reverse current inhibition caused by certain agents.
Activates the hERG channel without causing blockade.
Suppresses changes in membrane excitability.
Increases hERG current.
Inhibits action potential duration in ventricular muscle.
Reverses current inhibition induced by specific substances.
Encompass Procurement Services Non-distribution item offered as a customer accommodation; additional freight charges may apply. Learn More