ChemicalBook CAS DataBase List 877387-37-6

877387-37-6

Name	GSK5182
CAS	877387-37-6
Molecular Formula	C27H31NO3
Molecular Weight	417.55
MOL File	877387-37-6.mol

Chemical Properties

Melting point	168.8 °C(Solvent: Methanol)
Boiling point	567.6±50.0 °C(Predicted)
density	1.132±0.06 g/cm3(Predicted)
storage temp.	2-8°C
solubility	DMSO:54.5(Max Conc. mg/mL);130.52(Max Conc. mM) Ethanol:84.0(Max Conc. mg/mL);201.17(Max Conc. mM)
form	Solid
pka	10.27±0.15(Predicted)
color	Off-white to light yellow
InChIKey	ZVSFNBNLNLXEFQ-RQZHXJHFSA-N
SMILES	N(CCOc1ccc(cc1)\C(=C(\CCCO)/c3ccccc3)\c2ccc(cc2)O)(C)C

Safety Data

WGK Germany	WGK 3
Storage Class	6.1C - Combustible acute toxic Cat.3 toxic compounds or compounds which causing chronic effects
Hazard Classifications	Lact. Repr. 1A

Hazard Information

Uses

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)[1][2][3].

Biological Activity

GSK5182 is an orally available 4-hydroxy-tamoxifen (4-OHT) analog and a high affinity estrogen receptor-related receptor γ (ERRγ) inverse agonist (68% inhibition at 1 μM by reporter assay) with 25-fold reduced affinity and little antagonistic activity toward ERRα (No inhibition against 100 nM estradiol-induced reporter activity up to 1 μM). GSK5182 effectively inhibits ERRγ-dependent gene expression and biological functions both in cultures (1-10 μM) and in various animal studies in vivo (10-80 mg/kg i.p. or p.o. in rats and mice).

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^[3].

Animal Model:	db/db mice (male, 7-12-week-old), diet-induced obesity (DIO) mice^[3]
Dosage:	40 mg/kg
Administration:	Intraperitoneal injection; every day; 30 days for db/db mice, 25 days for DIO mice
Result:	Inhibited the transcriptional activity of ERRγ, suppressed hepatic glucose production through inhibition of hepatic gluconeogenesis.

IC 50

ERRγ: 79 nM (IC₅₀); Reactive Oxygen Species

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. DOI:10.1038/emm.2015.115
[2] Misra J, et al. ERRγ: a Junior Orphan with a Senior Role in Metabolism. Trends Endocrinol Metab. 2017 Apr;28(4):261-272. DOI:10.1016/j.tem.2016.12.005
[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. DOI:10.2337/db12-0946

Spectrum Detail

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