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GSK256073

Catalog No. T15432 CAS 862892-90-8

GSK256073 is an orally active GPR109A agonist. GSK256073 also is a long-lasting and non-flushing HCA2 (hydroxy-carboxylic acid receptor 2) full agonist (pEC50: 7.5). GSK256073 acutely improves glucose homeostasis via inhibition of lipolysis.

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GSK256073, CAS 862892-90-8

Pack Size	Availability	Price/USD
1 mg	In stock	$ 67.00
2 mg	In stock	$ 98.00
5 mg	In stock	$ 163.00
10 mg	In stock	$ 263.00
25 mg	In stock	$ 463.00
50 mg	In stock	$ 682.00
100 mg	In stock	$ 969.00
1 mL * 10 mM (in DMSO)	In stock	$ 178.00

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Purity: 98.03%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	GSK256073 is an orally active GPR109A agonist. GSK256073 also is a long-lasting and non-flushing HCA2 (hydroxy-carboxylic acid receptor 2) full agonist (pEC50: 7.5). GSK256073 acutely improves glucose homeostasis via inhibition of lipolysis.
Targets&IC50	HCA2 (hydroxy-carboxylic acid receptor 2):pEC50: 7.5
In vitro	GSK256073 (100 μM) suppresses cAMP elevation induced by isoprenaline (100 nM) in rat primary adipocytes. GSK256073 is approximately 10-fold more potent than niacin against human HCA2 (pEC50 value of 7.5 compared to 6.7 for niacin). In membranes prepared from Chinese hamster ovary cells expressing recombinant human HCA2, It has good activity versus the rat orthologue of HCA2 (pEC50 value of 6.9 compared to 6.4 for niacin) [2].
In vivo	GSK256073 (i.v.; 1-10 mg/kg) produces a dose-related decrease in NEFA, however, the enhanced in-ear temperature induced by 10 mg/kg i.v. GSK256073 is only 40% of that induced by 10 mg/kg i.v. niacin. GSK256073 (p.o.; 1, 30, and 100 mg/kg; in rat) displays that the fall in NEFA is of rapid onset and that the maximum is dose-related with inhibitions of 74, 81 and 88%, respectively. Although the duration was longer with a reduction of 91% still present 6 h post-dose at 10 mg/kg, triglycerides reduce is followed as a similar pattern [2].

Molecular Weight	256.69
Formula	C10H13ClN4O2
CAS No.	862892-90-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 16.67 mg/mL (64.94 mM), Sonication is recommended.

References and Literature

1. Dobbins RL, et al. GSK256073, a selective agonist of G-protein coupled receptor 109A (GPR109A) reduces serum glucose in subjects with type 2 diabetes mellitus.Diabetes Obes Metab. 2013 Nov;15(11):1013-21. 2. Sprecher D, et al. Discovery and characterization of GSK256073, a non-flushing hydroxy-carboxylic acid receptor 2 (HCA2) agonist.Eur J Pharmacol. 2015 Jun 5;756:1-7.

Citations

1. Zhu S, Yuan Q, Li X, et al.Molecular recognition of niacin and lipid-lowering drugs by the human hydroxycarboxylic acid receptor 2.Cell Reports.2023, 42(11).

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Membrane Protein-targeted Compound Library GPCR Compound Library NO PAINS Compound Library Anti-Metabolism Disease Compound Library Endocrinology-Hormone Compound Library Bioactive Compound Library Orally Active Compound Library

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Keywords

GSK256073 862892-90-8 Endocrinology/Hormones GPCR/G Protein Others GPR type 2 Inhibitor mellitus GSK-256073 HM74A HCA2 homeostasis GPCR T2DM dyslipidaemia GSK 256073 glucose HCAR2 diabete inhibit GPR109A PUMA-G inhibitor

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