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GSK1292263

Cat. No. M3321
GSK1292263 Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 110 In stock
10mg USD 150 In stock
50mg USD 490 In stock
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Quality Control
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
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 456.56
Formula C23H28N4O4S
CAS Number 1032823-75-8
Purity >99%
Solubility DMSO 29 mg/mL
Storage at -20°C
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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: GSK1292263 supplier, GPR, inhibitors

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