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
- Molecular Weight:
- 417.55
- MDL Number:
- MOL File:
- 877387-37-6.mol
| Product description | Number | Pack Size | Price |
| GSK5182 ≥95% (HPLC) | SML3150 | 5MG | $103.55 |
| GSK5182 ≥95% (HPLC) | SML3150 | 25MG | $438 |
| (E/Z)-GSK5182 98.90% | CS-0113537 | 10mg | $450 |
| GSK-5182 95.00% | BRS0009216 | 5MG | $451.36 |
| (E/Z)-GSK5182 98.90% | CS-0113537 | 50mg | $1200 |
| 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 |
| UNSPSC Code | 12352200 |
| NACRES | NA.77 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS08 |
|---|---|
| Signal word | Danger |
| Hazard statements | H360-H362 |
| Precautionary statements | P202-P260-P263-P264-P270-P308+P313 |
| 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 |
GSK5182 price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | SML3150 | GSK5182 ≥95% (HPLC) | 877387-37-6 | 5MG | $103.55 | 2025-07-31 | Buy |
| Sigma-Aldrich | SML3150 | GSK5182 ≥95% (HPLC) | 877387-37-6 | 25MG | $438 | 2025-07-31 | Buy |
| ChemScene | CS-0113537 | (E/Z)-GSK5182 98.90% | 877387-37-6 | 10mg | $450 | 2021-12-16 | Buy |
| American Custom Chemicals Corporation | BRS0009216 | GSK-5182 95.00% | 877387-37-6 | 5MG | $451.36 | 2021-12-16 | Buy |
| ChemScene | CS-0113537 | (E/Z)-GSK5182 98.90% | 877387-37-6 | 50mg | $1200 | 2021-12-16 | Buy |
GSK5182 Chemical Properties,Uses,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
GSK5182 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 33024 | 60 |
| Hubei Ipure Biology Co., Ltd | +8613367258412 | ada@ipurechemical.com | China | 10236 | 58 |
| HONG KONG IPURE BIOLOGY CO.,LIMITED | 86 18062405514 18062405514 | ada@ipurechemical.com | CHINA | 3461 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6391 | 58 |
| Hangzhou MolCore BioPharmatech Co.,Ltd. | +86-057181025280; +8617767106207 | sales@molcore.com | China | 49734 | 58 |
| Nantong HI-FUTURE Biology Co., Ltd. | +undefined18051384581 | sales@chemhifuture.com | China | 3135 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354; | support@targetmol.com | United States | 39042 | 58 |
| Wuhan Topule Biopharmaceutical Co., Ltd | +8618327326525 | masar@topule.com | China | 8467 | 58 |
| Shenyang Zhongshen Zekang Biomedical Technology Research Co., Ltd | +86-18341751992 +86-15382112998 | 757984502@qq.com | China | 892 | 58 |
| Aladdin Scientific | tp@aladdinsci.com | United States | 57505 | 58 |
