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

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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
InChIKey: ZVSFNBNLNLXEFQ-RQZHXJHFSA-N
SMILES: N(CCOc1ccc(cc1)\C(=C(\CCCO)/c3ccccc3)\c2ccc(cc2)O)(C)C

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Safety

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

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Danger

Hazard statements

H360May damage fertility or the unborn child

H362May cause harm to breast-fed children

Precautionary statements

P202Do not handle until all safety precautions have been read and understood.

P260Do not breathe dust/fume/gas/mist/vapours/spray.

P263Avoid contact during pregnancy/while nursing.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P308+P313IF exposed or concerned: Get medical advice/attention.

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML3150
Product name: GSK5182
Purity: ≥95% (HPLC)
Packaging: 5MG
Price: $103.55
Updated: 2025/07/31

Sigma-Aldrich

Product number: SML3150
Product name: GSK5182
Purity: ≥95% (HPLC)
Packaging: 25MG
Price: $438
Updated: 2025/07/31

ChemScene

Product number: CS-0113537
Product name: (E/Z)-GSK5182
Purity: 98.90%
Packaging: 5mg
Price: $280
Updated: 2021/12/16

ChemScene

Product number: CS-0113537
Product name: (E/Z)-GSK5182
Purity: 98.90%
Packaging: 10mg
Price: $450
Updated: 2021/12/16

American Custom Chemicals Corporation

Product number: BRS0009216
Product name: GSK-5182
Purity: 95.00%
Packaging: 5MG
Price: $451.36
Updated: 2021/12/16

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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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GSK5182 Suppliers

China 58 United States 5 Global 63

Nanjing Chemlin Chemical Co., Ltd

Tel: 025-83697070 13913916777;
Fax: +86-25-83453306
Email: info@chemlin.com.cn
Country: China
ProdList: 15724
Advantage: 64

Shanghai Lollane Biological Technology Co.,Ltd.

Tel: 021-52996696，15000506266 15000506266
Fax: +86-21-52996696
Country: China
ProdList: 4795
Advantage: 55

Shanghai EFE Biological Technology Co., Ltd.

Tel: 021-65675885 18964387627
Fax: 021-65675885
Email: info@efebio.com
Country: China
ProdList: 9803
Advantage: 58

Shanghai YuanYe Biotechnology Co., Ltd.

Tel: 021-61312847; 18021002903
Fax: QQ:3008007432
Email: 3008007409@qq.com
Country: China
ProdList: 71826
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Tianjin Kailiqi Biotechnology Co., Ltd.

Tel: 15076683720
Fax: 022-23754520
Email: klq@cw-bio.com
Country: China
ProdList: 9377
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ShangHai Biochempartner Co.,Ltd

Tel: 177-54423994 17754423994
Fax: QQ:2853530913
Email: 2853530910@QQ.com
Country: China
ProdList: 8000
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Shanghai Chaolan Chemical Technology Center

Tel: 021-QQ：65489617 15618227136
Fax: 21-5161 9052
Email: Sales@ATKchemical.com
Country: China
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Shanghai Jizhi Biochemical Technology Co. Ltd.

Tel: 021-4009004166/18616739031 18616739031
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Beijing Minruida Technology Co., Ltd.

Tel: 010-82387566 18001021521;
Fax: 82387566-801
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Country: China
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Chongqing Zhisheng Technology Co., Ltd.

Tel: 023-67586781 17783613370
Fax: QQ 2636861874
Email: 2636861874@qq.com
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877387-37-6, GSK5182Related Search:

GSK5182

CS-2620

(Z)-4-(1-(4-(2-(dimethylamino)ethoxy)phenyl)-5-hydroxy-2-phenylpent-1-en-1-yl)phenol

(E/Z)-GSK5182

Benzenebutanol, δ-[[4-[2-(dimethylamino)ethoxy]phenyl](4-hydroxyphenyl)methylene]-, (δZ)-

4-[(Z)-1-[4-[2-(Dimethylamino)ethoxy]phenyl]-5-hydroxy-2-phenylpent-1-enyl]phenol

inhibit,GSK-5182,GSK5182,Reactive Oxygen Species,GSK 5182,Estrogen Receptor/ERR,Inhibitor

(E/Z)GSK5182,(E/Z) GSK5182,(E/Z)-GSK-5182

GSK5182, 10 mM in DMSO

GSK5182 ，S3449

877387-37-6