GSK5182 free base · Synonyms: GSK-5182 · GSK 5182

GSK5182 is a highly selective and orally active inverse agonist of estrogen-related receptor γ.

For research use only. Not for human or veterinary use.

Target Estrogen Receptor/ERR Reactive Oxygen Species (ROS)

Research area Cardiovascular Disease Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

GSK5182 structure

CAS No.: 877387-37-6

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
100 mg	USD 480.00	BP-02138-100mg	In stock	Get quote
250 mg	USD 950.00	BP-02138-250mg	In stock	Get quote
500 mg	USD 1,500.00	BP-02138-500mg	In stock	Get quote
1 g	USD 2,400.00	BP-02138-1g	In stock	Get quote
2 g	USD 3,800.00	BP-02138-2g	In stock	Get quote

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Description

GSK5182 is a highly selective and orally active inverse agonist of estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM. GSK5182 does not interact with other nuclear receptors, including ERRα or ERα. GSK5182 also induces reactive oxyen species (ROS) generation in hepatocellular carcinoma (HCC) .

Biological activity

In Vitro GSK5182 (0-20 μM; 0-hours; PLC/PRF/5 cells) treatment leads to a significant and dose-dependent reduction in the number of proliferating PLC/PRF/5 cells. GSK5182 (0-20 μM; 24 hours; PLC/PRF/5 cells) treatment also causes a dose-dependent increase in the expression of p21 and p27 while at the same time reducing the level of phosphorylated retinoblastoma protein (p-pRb). GSK5182 (10-20 μM; PLC/PRF/5 cells) treatment induces cell cycle arrest at G1 phase, which in turn induces a corresponding dose-dependent reduction in the percentage of cells in S phase. In Vivo GSK5182 (40 mg/kg; intraperitoneal injection; every day; 25 or 30 days; db/db mice, diet-induced obesity mice) specifically inhibits the transcriptional activity of ERRγ, and suppresses hepatic glucose production through inhibition of hepatic gluconeogenesis. GSK5182 elicits anti-diabetic effects in mouse models via negative regulation of the hepatic gluconeogenesis program. GSK5182 normalizes hyperglycemia mainly through inhibition of hepatic glucose production.

Identifiers

SMILES: CN(C)CCOC1=CC=C(C=C1)C(=C(\CCCO)C1=CC=CC=C1)\C1=CC=C(O)C=C1
InChIKey: ZVSFNBNLNLXEFQ-RQZHXJHFSA-N

Specifications

MW (average): 417.5399
Formula: C₂₇H₃₁NO₃
CAS No.: 877387-37-6
Physical state: Solid
Color: White to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 3 years; 4℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO,>10mg/mL, not in water

Documents

References

[1].Kim JH, et al. Estrogen-related receptor γ is upregulated in liver cancer and its inhibition suppresses livercancer cell proliferation via induction of p21 and p27. Exp Mol Med. 2016 Mar 4;48:e213.

[2]. Misra J, et al. ERRγ: a Junior Orphan with a Senior Role in Metabolism. Trends Endocrinol Metab. 2017 Apr;28(4):261-272.

[3].Kim DK, et al. Inverse agonist of nuclear receptor ERRγ mediates antidiabetic effect through inhibition of hepatic gluconeogenesis. Diabetes. 2013 Sep;62(9):3093-102.

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