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GSK1292263

Cat. No. M3321
GSK1292263 Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
2mg USD 50  USD50 In stock
5mg USD 80  USD80 In stock
10mg USD 120  USD120 In stock
25mg USD 210  USD210 In stock
50mg USD 380  USD380 In stock
100mg USD 550  USD550 In stock
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Quality Control & Documentation
Biological Activity

GSK1292263 is a novel GPR119 receptor agonist used for the treatment of type 2 diabetes. In the intravenous glucose tolerance test, significant increases in the peak insulin response and insulin AUC (0-15 min) of 30-60% were reported in the GSK1292263 treatment group, compared with values in the vehicle control cohort. This insulin upregulation correlated with a significant increase in the glucose disposal rate.

Customer Product Validations & Biological Datas
Source Eur J Pharmacol (2017). Figure 2. GSK1292263
Method i.v.
Cell Lines mice
Concentrations 30 mg/kg
Incubation Time 0 to 4 h
Results Our findings also demonstrated that all three GPR119 agonists (APD668, GSK1292263 and MBX2982) tested improved fat tolerance suggesting a GPR119 receptor mediated effect
Protocol (for reference only)
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models male Sprague-Dawley rats
Formulation 0.9% sodium chloride solution
Dosages 3-30 mg/kg
Administration
Chemical Information
Molecular Weight 456.56
Formula C23H28N4O4S
CAS Number 1032823-75-8
Solubility (25°C) DMSO 22 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] Ji Hye Im, et al. GPR119 agonist enhances gefitinib responsiveness through lactate-mediated inhibition of autophagy

[2] Jin Won Yang, et al. GPR119: a promising target for nonalcoholic fatty liver disease

[3] Derek J Nunez, et al. Gut hormone pharmacology of a novel GPR119 agonist (GSK1292263), metformin, and sitagliptin in type 2 diabetes mellitus: results from two randomized studies

[4] Sang-Uk Kang. GPR119 agonists: a promising approach for T2DM treatment? A SWOT analysis of GPR119

[5] Joseph W Polli, et al. Evaluation of drug interactions of GSK1292263 (a GPR119 agonist) with statins: from in vitro data to clinical study design

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