Ro 28-1675 is an effective allosteric GK activator (IC50: 0.24± 0.0019 uM).

GK:54 nM (EC50)

Ro 28-1675 (50 mg/Kg; p.o.;) treatment to male C57B1/6J mice caused a statistically significant reduction in fasting glucose levels and improvement in glucose tolerance relative to the vehicle-treated animals. Glucokinase activator The R stereoisomer Ro 28-1675 activated GK with an SC1.5 of 0.24 uM, while the S isomer did not activate GK up to 10 uM. A comparison of rat PK parameters indicated that Ro 28-1675 displayed lower clearance and higher oral bioavailability compared to 9a. Ro 28-1675 reduced fasting and postprandial glucose levels following an OGTT following a single oral dose, was well tolerated and displayed no adverse effects related to drug administration other than hypoglycemia at the maximum dose (400 mg) [1]