GSK256073

SKU: orb1308250

Description

GSK256073 is a potent, orally bioavailable, and non-flushing full agonist of the hydroxy-carboxylic acid receptor 2 (HCA2/GPR109A). It acutely improves glucose homeostasis by inhibiting lipolysis, making it a valuable research tool for studying metabolic disorders such as type 2 diabetes and dyslipidemia in both in vitro and in vivo models.

Research Area

Metabolism Research, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 862892-90-8
• MW: 256.69
• Purity: 98.46% (May vary between batches)
• Formula: C₁₀H₁₃ClN₄O₂
• SMILES: CCCCCn1c2nc(Cl)[nH]c2c(=O)[nH]c1=O
• Target: GPCR
• Solubility: 10% DMSO+90% Corn Oil:1.5 mg/mL (5.84 mM);DMSO:16.67 mg/mL (64.94 mM)

Bioactivity

• Target IC50:
  HCA2 (hydroxy-carboxylic acid receptor 2):pEC50: 7.5
• 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 .
• 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) .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, Inhibitor, GPR109A, GPR109A (G-protein coupled receptor 109A), glucose, GSK 256073, GSK256073, GSK-256073, GPCR, HCAR2, HCA2, HCA2 (hydroxy-carboxylic acid receptor 2), HM74A, mellitus, homeostasis, dyslipidaemia, diabete, PUMA-G, type 2, T2DM

Compound Identifiers

PubChem CID

46215799