TMG-123

Cat. No. M31409

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Quality Control & Documentation

Purity: >99.0%
COA
MSDS

Product Information

Biological Activity

TMG-123 is a glucokinase (GK) activator that can be used in studies related to type 2 diabetes.

Chemical Information

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
K_m factor	3	6	12	8	5	20

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B K_m
	Animal A K_m

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 K_m factor for a mouse and then divide by the K_m factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Yoshinori Tsumura, et al. PLoS One. Disruptions in hepatic glucose metabolism are involved in the diminished efficacy after chronic treatment with glucokinase activator

[2] Taiki Kobayashi, et al. J Toxicol Sci. A novel glucokinase activator TMG-123 causes long-lasting hypoglycemia and impairs spermatogenesis irreversibly in rats

[3] Yoshinori Tsumura, et al. PLoS One. TMG-123, a novel glucokinase activator, exerts durable effects on hyperglycemia without increasing triglyceride in diabetic animal models

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MK-0941 free base MK-0941 free base is an orally active glucokinase activator, with EC50s of 240 and 65 nM for recombinant human glucokinase in the presence of 2.5 and 10 mM glucose, respectively. MK-0941 free base exhibits strong glucose-lowering activity and is a potential therapeutic agent for treatment of type 2 diabetes.
AMG-1694 AMG-1694 is a potent glucokinase–glucokinase regulatory protein (GK-GKRP) disruptors and promotes the dissociation of the GK-GKRP complex with an IC50 of 7 nM, indirectly increasing GK enzymatic activity. AMG-1694 potently reverses the inhibitory effect of GKRP on GK activity and promotes GK translocation. AMG-1694 normalizes blood glucose levels in several rodent models of diabetes and lowes blood glucose restricted to diabetic and not normoglycaemic animals.

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Signaling Pathways

TMG-123

Quality Control & Documentation

Biological Activity

Chemical Information

Conversion of different model animals based on BSA (PMID: 27057123)

References

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