| Description | Ro 28-1675 is an effective allosteric GK activator (IC50: 0.24± 0.0019 uM). |
| In vitro | 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] |
| Target activity | GK:54 nM (EC50) |
| Synonyms | Ro 28-1675 |
| molecular weight | 378.51 |
| Molecular formula | C18H22N2O3S2 |
| CAS | 300353-13-3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 50 mg/mL (132.10 mM), Sonication is recommended. |
| References | 1. Fenner D, et al. Generation of N-ethyl-N-nitrosourea (ENU) diabetes models in mice demonstrates genotype-specific action ofglucokinase activators. J Biol Chem. 2011 Nov 11;286(45):39560-39572. 2. Haynes NE, et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N-thiazol-2-yl-propionamide (RO0281675). |