GSK5182

SKU: orb1298992

Description

GSK5182 is a potent and selective inverse agonist of estrogen-related receptor γ (ERRγ), exhibiting an IC50 of 79 nM. This small molecule is a valuable research tool for studying ERRγ's role in metabolic regulation, energy homeostasis, and related diseases in both cellular and animal models.

Research Area

Immunology & Inflammation, Metabolism Research, Signal Transduction

Key Properties

• CAS Number: 877387-37-6
• MW: 417.54
• Purity: 97.63% (May vary between batches)
• Formula: C₂₇H₃₁NO₃
• SMILES: C(=C(/CCCO)\C1=CC=CC=C1)(\C2=CC=C(OCCN(C)C)C=C2)/C3=CC=C(O)C=C3
• Target: Estrogen/progestogen Receptor,ROS,Reactive Oxygen Species,Estrogen Receptor/ERR
• Solubility: DMSO:80 mg/mL (191.6 mM)

Bioactivity

• Target IC50:
  ERRγ:79 nM (IC50)
• In Vivo:
  a hyperinsulinemic-euglycemic clamp study and long-term studies of the antidiabetic effects of GSK5182, the ERRγ-specific inverse agonist, in db/db and DIO mice demonstrated that GSK5182 normalizes hyperglycemia mainly through inhibition of hepatic glucose production.
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• In Vitro:
  Small interfering RNA (siRNA)-mediated knockdown of ERRγ (siRNA-ERRγ) or an ERRγ inverse agonist, GSK5182, were also used to examine the effects of ERRγ inhibition on the proliferation and growth of a human hepatoma cell line, PLC/PRF/5.
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• Cell Research:
  Cell Line:The human hepatoma cell line PLC/PRF/5. Concentration:0 μM, 10 μM, 20 μM. Incubation Time:0 hour, 24 hours, 48 hours, 72 hours

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Reactive Oxygen Species, ReactiveOxygenSpecies, progestogen Receptor, progestogenReceptor, inhibit, Inhibitor, ERR, ERRγ, GSK 5182, Estrogen Receptor, Estrogen Receptor/ERR, EstrogenReceptor, GSK5182, GSK-5182

Compound Identifiers

PubChem CID

6852176