1. GPCR/G Protein
  2. GPR109A
  3. GSK256073

GSK256073 

Cat. No.: HY-119222
Handling Instructions

GSK256073 is a potent, selective and orally active GPR109A agonist and a long-lasting and non-flushing HCA2 full agonist with a pEC50 of 7.5 (human HCA2). GSK256073 acutely improves glucose homeostasis via inhibition of lipolysis and has the potential for the study of type 2 diabetes mellitus (T2DM)and dyslipidemia. GPR109A: G-protein coupled receptor 109A; HCA2: hydroxy-carboxylic acid receptor 2

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GSK256073 Chemical Structure

GSK256073 Chemical Structure

CAS No. : 862892-90-8

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Description

GSK256073 is a potent, selective and orally active GPR109A agonist and a long-lasting and non-flushing HCA2 full agonist with a pEC50 of 7.5 (human HCA2). GSK256073 acutely improves glucose homeostasis via inhibition of lipolysis and has the potential for the study of type 2 diabetes mellitus (T2DM)and dyslipidemia[1][2]. GPR109A: G-protein coupled receptor 109A; HCA2: hydroxy-carboxylic acid receptor 2

IC50 & Target

IC50: GPR109A (G-protein coupled receptor 109A); HCA2 (hydroxy-carboxylic acid receptor 2)[1][2]

In Vitro

GSK256073 is approximately 10-fold more potent than niacin against human HCA2 (pEC50 value of 7.5 compared to 6.7 for niacin), has good activity versus the rat orthologue of HCA2 (pEC50 value of 6.9 compared to 6.4 for niacin) in membranes prepared from Chinese hamster ovary cellsexpressing recombinant human HCA2[2].
GSK256073 (100 μM) suppresses cAMP elevation induced by isoprenaline (100 nM) in rat primary adipocytes[2].

In Vivo

GSK256073 (oral adminstration; 1, 30 and 100 mg/kg; in rat) shows that the fall in NEFA is of rapid onset and that the maximum is dose-related with inhibitions of 74, 81 and 88%, respectively. Triglycerides decrease is followed as a similar pattern,although the duration was longer with a decrease of 91% still present 6 h post dose at 10 mg/kg[2].
GSK256073 (intravenous injection; 1-10 mg/kg) produces a dose related decrease in NEFA. However, the increase in ear temperature induced by 10 mg/kg i.v. GSK256073 is only 40% of that induced by 10 mg/kg i.v. niacin[2].

Animal Model: SD rat[2]
Dosage: 1, 30 and 100 mg/kg
Administration: Oral adminstration
Result: Inhibited NEFA expression as a dose-dependent manner.
Animal Model: Guinea pigs[2]
Dosage: 10 mg/kg
Administration: Intravenous injection
Result: Had the antilipolytic and flushing effects as a HCA2 agonist.
Molecular Weight

256.69

Formula

C₁₀H₁₃ClN₄O₂

CAS No.

862892-90-8

SMILES

O=C(N(C1=C2NC(Cl)=N1)CCCCC)NC2=O

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

GSK256073GSK 256073GSK-256073GPR109AHM74APUMA-GHCA2HCAR2 GPCRdyslipidaemiatype 2diabetemellitusglucoseT2DMhomeostasisInhibitorinhibitorinhibit

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GSK256073
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HY-119222
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