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

GSK256073 

Cat. No.: HY-119222 Purity: 99.27%
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

For research use only. We do not sell to patients.

GSK256073 Chemical Structure

GSK256073 Chemical Structure

CAS No. : 862892-90-8

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5 mg USD 300 In-stock
Estimated Time of Arrival: December 31
10 mg USD 450 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1200 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
250 mg USD 2500 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Clinical Trial
Molecular Weight

256.69

Formula

C₁₀H₁₃ClN₄O₂

CAS No.

862892-90-8

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 16.67 mg/mL (64.94 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.8957 mL 19.4787 mL 38.9575 mL
5 mM 0.7791 mL 3.8957 mL 7.7915 mL
10 mM 0.3896 mL 1.9479 mL 3.8957 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 1.67 mg/mL (6.51 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.27%

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Keywords:

GSK256073GSK 256073GSK-256073GPR109AHM74APUMA-GHCA2HCAR2 GPCRdyslipidaemiatype 2diabetemellitusglucoseT2DMhomeostasisInhibitorinhibitorinhibit

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GSK256073
Cat. No.:
HY-119222
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