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300353-13-3

300353-13-3 Structure

300353-13-3 Structure
IdentificationBack Directory
[Name]

(2R)-3-Cyclopentyl-2-[4-(methanesulfonyl)phenyl]-N-(thiazol-2-yl)propionamide
[CAS]

300353-13-3
[Synonyms]

Ro 0281675
Ro 28-1675
RO 028-1675;RO 0281675
RO 28-1675 - RO 28-0450, (R)-
(2R)-3-Cyclopentyl-2-[4-(methanesulfonyl)phenyl]-N-(thiazol-2-yl)propionamide
BenzeneacetaMide, α-(cyclopentylMethyl)-4-(Methylsulfonyl)-N-2-thiazolyl-, (αR)-
[Molecular Formula]

C18H22N2O3S2
[MOL File]

300353-13-3.mol
[Molecular Weight]

378.51
Chemical PropertiesBack Directory
[density ]

1.306
[storage temp. ]

Store at -20°C
[solubility ]

DMSO : 50 mg/mL (132.10 mM; Need ultrasonic)
[form ]

Powder
[pka]

8.65±0.50(Predicted)
[color ]

White to off-white
Hazard InformationBack Directory
[Definition]

ChEBI: (2R)-3-cyclopentyl-2-(4-methylsulfonylphenyl)-N-(2-thiazolyl)propanamide is a member of acetamides.
[Biological Activity]

RO-28-1675 is a potent allosteric activator of glucokinase with EC50 of 54 nM. It can be used in type 2 diabetes research.
[in vitro]

RO-28-1675 can reverse the inhibitory action of the human glucokinase regulatory protein (GKRP).

[in vivo]

RO-28-1675 (50 mg/kg; po) reduces blood glucose levels in wild-type C57BL/6J mice.
RO-28-1675 (10 mg/kg; po) displays lower clearance and higher oral bioavailability.

Animal Model: 10 weeks old male C57BL/6J mice
Dosage: 50 mg/kg
Administration: Oral administration
Result: Reduced blood glucose levels.
Animal Model: C57BL/6J mice
Dosage: 10 mg/kg
Administration: Oral administr ation
Result: AUC 0-inf (5150 ng? h/mL), C max (1140 μg/mL) , T max (3.3 hours ), F po (92.8%) with 10 mg/kg orally administered.
[target]

EC50: 54 nM (glucokinase)

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