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GSK256073

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Catalog No. T15432Cas No. 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.

GSK256073

GSK256073

🥰Excellent
Purity: 98.03%
Catalog No. T15432Cas No. 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.
Pack SizePriceAvailabilityQuantity
1 mg63 €In Stock
2 mg93 €In Stock
5 mg154 €In Stock
10 mg249 €In Stock
25 mg439 €In Stock
50 mg647 €In Stock
100 mg920 €In Stock
1 mL x 10 mM (in DMSO)169 €In Stock
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Purity:98.03%
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Product Introduction

Bioactivity
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].
Chemical Properties
Molecular Weight256.69
FormulaC10H13ClN4O2
Cas No.862892-90-8
SmilesCCCCCn1c2nc(Cl)[nH]c2c(=O)[nH]c1=O
Relative Density.1.373 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 16.67 mg/mL (64.94 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM3.8957 mL19.4787 mL38.9575 mL194.7875 mL
5 mM0.7791 mL3.8957 mL7.7915 mL38.9575 mL
10 mM0.3896 mL1.9479 mL3.8957 mL19.4787 mL
20 mM0.1948 mL0.9739 mL1.9479 mL9.7394 mL
50 mM0.0779 mL0.3896 mL0.7791 mL3.8957 mL

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