| Bioactivity | 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]. | ||||||||||||
| Target | EC50: 54 nM (glucokinase) | ||||||||||||
| Invitro | RO-28-1675 can reverse the inhibitory action of the human glucokinase regulatory protein (GKRP)[2]. | ||||||||||||
| In Vivo | 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]. Animal Model: | ||||||||||||
| Name | RO-28-1675 | ||||||||||||
| CAS | 300353-13-3 | ||||||||||||
| Formula | C18H22N2O3S2 | ||||||||||||
| Molar Mass | 378.51 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| 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. |
RO-28-1675
CAS: 300353-13-3 F: C18H22N2O3S2 W: 378.51
RO-28-1675 is a potent allosteric glucokinase (GK) activator with an EC50 of 54 nM. RO-28-1675 can be used for the resea
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