For research use only. Not for therapeutic Use.
RO-28-1675 is a potent allosteric glucokinase (GK) activator with an EC50 of 54 nM. RO-28-1675 can be used for the research of type 2 diabetes[1][2].
RO-28-1675 can reverse the inhibitory action of the human glucokinase regulatory protein (GKRP)[2].
RO-28-1675 (50 mg/kg; p.o.) reduces blood glucose levels in wild-type C57BL/6J mice[2].
RO-28-1675 exhibits high oral bioavailability (mice 92.8%) and Cmax (1140 μg/mL) following oral administration (10 mg/kg)[1].
| Catalog Number | I003041 |
| CAS Number | 300353-13-3 |
| Synonyms | (2R)-3-cyclopentyl-2-(4-methylsulfonylphenyl)-N-(1,3-thiazol-2-yl)propanamide |
| Molecular Formula | C18H22N2O3S2 |
| Purity | ≥95% |
| InChI | InChI=1S/C18H22N2O3S2/c1-25(22,23)15-8-6-14(7-9-15)16(12-13-4-2-3-5-13)17(21)20-18-19-10-11-24-18/h6-11,13,16H,2-5,12H2,1H3,(H,19,20,21)/t16-/m1/s1 |
| InChIKey | NEQSWPCDHDQINX-MRXNPFEDSA-N |
| SMILES | CS(=O)(=O)C1=CC=C(C=C1)C(CC2CCCC2)C(=O)NC3=NC=CS3 |
| Reference | [1]. Nancy-Ellen Haynes, et al. Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N-thiazol-2-yl-propionamide (RO0281675). J Med Chem. 2010 May 13;53(9):3618-25. [2]. Joseph Grimsby, et al. Allosteric activators of glucokinase: potential role in diabetes therapy. Science. 2003 Jul 18;301(5631):370-3. |
