GSK5182

Catalog No.S3449 Batch:S344901

Technical Data

Formula	C₂₇H₃₁NO₃
Molecular Weight	417.54	CAS No.	877387-37-6
Solubility (25°C)*	In vitro	DMSO	84 mg/mL (201.17 mM)
		Ethanol	84 mg/mL (201.17 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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

GSK5182, a small-molecule ERRγ inverse agonist, inhibits pro-inflammatory cytokine-induced catabolic factors in mouse articular chondrocytes.^[1]

In vivo

GSK5182 significantly reduces cartilage degeneration in ERRγ-overexpressing mice administered intra-articular Ad-Esrrg.^[1]

Protocol (from reference)

Cell Assay:^{^[1]}	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.
Animal Study:^{^[1]}	Animal Models Cartilage-specific ERRγ Tg mice (Col2a1-Esrrg) Dosages -- Administration i.a.

Cell Assay:^{^[1]}

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.

Animal Study:^{^[1]}

Animal Models
Cartilage-specific ERRγ Tg mice (Col2a1-Esrrg)
Dosages
--
Administration
i.a.

References

[1] Yunhui Min, et al. Pharmaceuticals (Basel). 2020 Nov 27;13(12):429.

Selleck's GSK5182 has been cited by 1 publication

Cross-ancestry genome-wide analysis of atrial fibrillation unveils disease biology and enables cardioembolic risk prediction [ Nat Genet, 2023, 55(2):187-197]	PubMed: 36653681

Cross-ancestry genome-wide analysis of atrial fibrillation unveils disease biology and enables cardioembolic risk prediction [ Nat Genet, 2023, 55(2):187-197]

PubMed: 36653681

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SHIPPING AND STORAGE
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