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RO-28-1675

Cat. No. M14437
RO-28-1675 Structure
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Biological Activity

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.

Chemical Information
Molecular Weight 378.51
CAS Number 300353-13-3
Solubility (25°C) DMSO 50 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Sara Langer, et al. The novel GCK variant p.Val455Leu associated with hyperinsulinism is susceptible to allosteric activation and is conducive to weight gain and the development of diabetes

[2] Sara Langer, et al. 6-Phosphofructo-2-kinase/fructose-2,6-bisphosphatase and small chemical activators affect enzyme activity of activating glucokinase mutants by distinct mechanisms

[3] Sefaa Al-aryahi, et al. Atherogenic, fibrotic and glucose utilising actions of glucokinase activators on vascular endothelium and smooth muscle

[4] Manojit Pal. Medicinal chemistry approaches for glucokinase activation to treat type 2 diabetes

[5] Hadi Al-Hasani, et al. Two birds with one stone: novel glucokinase activator stimulates glucose-induced pancreatic insulin secretion and augments hepatic glucose metabolism

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Keywords: RO-28-1675 supplier, Glucokinase (GK), inhibitors, activators

 
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