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GSK256073

Cat. No. M45123

All AbMole products are for research use only, cannot be used for human consumption.

GSK256073 Structure

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Quality Control & Documentation
Biological Activity

GSK256073 is a potent, selective, orally active GPR109A agonist and a potent and persistent HCA2 agonist with a pEC50 of 7.5 (Human HCA2). In addition, GSK256073 significantly improves glucose homeostasis by inhibiting lipid degradation and has potential for the study of type 2 diabetes mellitus (T2DM) and dyslipidemia.

Chemical Information
Molecular Weight 256.69
Formula C10H13ClN4O2
CAS Number 862892-90-8
Form Solid
Solubility (25°C) DMSO 16.67 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Jae-Hyun Park, et al. Nat Commun. Structural basis for ligand recognition and signaling of hydroxy-carboxylic acid receptor 2

[2] Eric J Olson, et al. Clin Pharmacol Drug Dev. A Randomized, Placebo-Controlled Trial to Assess the Effects of 8 Weeks of Administration of GSK256073, a Selective GPR109A Agonist, on High-Density Lipoprotein Cholesterol in Subjects With Dyslipidemia

[3] Dennis Sprecher, et al. Eur J Pharmacol. Discovery and characterization of GSK256073, a non-flushing hydroxy-carboxylic acid receptor 2 (HCA2) agonist

[4] Robert Dobbins, et al. Eur J Pharmacol. GSK256073 acutely regulates NEFA levels via HCA2 agonism but does not achieve durable glycaemic control in type 2 diabetes. A randomised trial

[5] R L Dobbins, et al. Diabetes Obes Metab. GSK256073, a selective agonist of G-protein coupled receptor 109A (GPR109A) reduces serum glucose in subjects with type 2 diabetes mellitus

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Keywords: GSK256073 supplier, GPR/FFAR, inhibitors, activators

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