Home Endocrinology & Hormones Estrogen/progestogen Receptor agonist GSK5182 For research use only.

GSK5182

GSK5182, 4-hydroxytamoxifen analog, is a specific inverse agonist of estrogen-related receptor γ (ERRγ) that inhibits pro-inflammatory cytokine-induced catabolic factors.

GSK5182 Chemical Structure

GSK5182 Chemical Structure

CAS No. 877387-37-6

Purity & Quality Control

Batch: S344901 DMSO]84 mg/mL]false]Ethanol]84 mg/mL]false]Water]Insoluble]false Purity: 99.85%
99.85

GSK5182 Related Products

Signaling Pathway

Estrogen/progestogen Receptor Signaling Pathways

Estrogen/progestogen Receptor Signaling Pathway

Biological Activity

Description GSK5182, 4-hydroxytamoxifen analog, is a specific inverse agonist of estrogen-related receptor γ (ERRγ) that inhibits pro-inflammatory cytokine-induced catabolic factors.
Targets
ERRγ [1]
In vitro
In vitro

GSK5182, a small-molecule ERRγ inverse agonist, inhibits pro-inflammatory cytokine-induced catabolic factors in mouse articular chondrocytes.[1]
Cell Research Cell lines Mouse articular chondrocytes
Concentrations 2.5, 5, 10 μM
Incubation Time 24 h
Method

Mouse articular chondrocytes (3×10<sup>5</sup>) were cultured for two days, infected with various concentrations of Ad-Esrrg adenoviruses [200 800 MOI (multiplicity of infection)] for 2 h, and cultured in the presence or absence of GSK5182 (2.5-10 μM) for an additional 24 h. Cells were treated with various inflammatory cytokines (IL-1β; 0.1-1 ng/mL, IL-6; 10-50 ng/mL, and TNF-α; 10-50 ng/mL) for 24 h.
In Vivo
In vivo

GSK5182 significantly reduces cartilage degeneration in ERRγ-overexpressing mice administered intra-articular Ad-Esrrg.[1]
Animal Research Animal Models Cartilage-specific ERRγ Tg mice (Col2a1-Esrrg)
Dosages --
Administration i.a.

Chemical Information & Solubility

Molecular Weight 417.54 Formula

C27H31NO3
CAS No. 877387-37-6 SDF --
Smiles CN(C)CCOC1=CC=C(C=C1)/C(=C(/CCCO)C2=CC=CC=C2)C3=CC=C(O)C=C3
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 84 mg/mL ( (201.17 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 84 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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