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

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

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 220 In-stock
Solution
10 mM * 1 mL in DMSO USD 220 In-stock
Solid
5 mg USD 200 In-stock
10 mg USD 320 In-stock
25 mg USD 560 In-stock
50 mg USD 860 In-stock
100 mg USD 1250 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

GSK256073 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE GSK256073

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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].

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

GSK256073 Related Antibodies
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 inhibition 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].

MedChemExpress (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.
Appearance

Solid

Color

White to off-white

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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 16.67 mg/mL (64.94 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

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

    This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.11%

COA (248 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.8957 mL 19.4787 mL 38.9575 mL 97.3937 mL
5 mM 0.7791 mL 3.8957 mL 7.7915 mL 19.4787 mL
10 mM 0.3896 mL 1.9479 mL 3.8957 mL 9.7394 mL
15 mM 0.2597 mL 1.2986 mL 2.5972 mL 6.4929 mL
20 mM 0.1948 mL 0.9739 mL 1.9479 mL 4.8697 mL
25 mM 0.1558 mL 0.7791 mL 1.5583 mL 3.8957 mL
30 mM 0.1299 mL 0.6493 mL 1.2986 mL 3.2465 mL
40 mM 0.0974 mL 0.4870 mL 0.9739 mL 2.4348 mL
50 mM 0.0779 mL 0.3896 mL 0.7791 mL 1.9479 mL
60 mM 0.0649 mL 0.3246 mL 0.6493 mL 1.6232 mL
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GSK256073 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GSK256073862892-90-8GSK 256073GSK-256073GPR109AHM74APUMA-GHCA2HCAR2 GPCRdyslipidaemiatype 2diabetemellitusglucoseT2DMhomeostasisInhibitorinhibitorinhibit

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