GSK5182
- Product Name
- GSK5182
- CAS No.
- 877387-37-6
- Chemical Name
- GSK5182
- Synonyms
- CS-2620;GSK5182;(E/Z)-GSK5182;GSK5182 ，S3449;GSK5182, 10 mM in DMSO;(E/Z)GSK5182,(E/Z) GSK5182,(E/Z)-GSK-5182;4-[(Z)-1-[4-[2-(Dimethylamino)ethoxy]phenyl]-5-hydroxy-2-phenylpent-1-enyl]phenol;(Z)-4-(1-(4-(2-(dimethylamino)ethoxy)phenyl)-5-hydroxy-2-phenylpent-1-en-1-yl)phenol;Benzenebutanol, δ-[[4-[2-(dimethylamino)ethoxy]phenyl](4-hydroxyphenyl)methylene]-, (δZ)-;inhibit,GSK-5182,GSK5182,Reactive Oxygen Species,GSK 5182,Estrogen Receptor/ERR,Inhibitor
- CBNumber
- CB33357971
- Molecular Formula
- C27H31NO3
- Formula Weight
- 417.55
- MOL File
- 877387-37-6.mol
GSK5182 Property
- 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) - pka
- 10.27±0.15(Predicted)
- form
- Solid
- color
- Off-white to light yellow
N-Bromosuccinimide Price
- Product number
- SML3150
- Product name
- GSK5182
- Purity
- ≥95% (HPLC)
- Packaging
- 5MG
- Price
- $103.55
- Updated
- 2025/07/31
- Product number
- SML3150
- Product name
- GSK5182
- Purity
- ≥95% (HPLC)
- Packaging
- 25MG
- Price
- $438
- Updated
- 2025/07/31
- Product number
- CS-0113537
- Product name
- (E/Z)-GSK5182
- Purity
- 98.90%
- Packaging
- 10mg
- Price
- $450
- Updated
- 2021/12/16
- Product number
- BRS0009216
- Product name
- GSK-5182
- Purity
- 95.00%
- Packaging
- 5MG
- Price
- $451.36
- Updated
- 2021/12/16
- Product number
- CS-0113537
- Product name
- (E/Z)-GSK5182
- Purity
- 98.90%
- Packaging
- 50mg
- Price
- $1200
- Updated
- 2021/12/16
GSK5182 Chemical Properties,Usage,Production
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
GSK5182 Preparation Products And Raw materials
Raw materials
Preparation Products
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