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SML3150

Sigma-Aldrich

GSK5182

≥95% (HPLC)

Synonyme(s) :

(δZ)-δ-[[4-[2-(Dimethylamino)ethoxy]phenyl](4-hydroxyphenyl)methylene]benzenebutanol, 4-[(Z)-1-[4-(2-Dimethylaminoethyloxy)phenyl]-hydroxy-2-phenylpent-1-enyl]phenol, GSK 5182, GSK-5182

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About This Item

Formule empirique (notation de Hill) :
C27H31NO3
Numéro CAS:
877387-37-6
Poids moléculaire :
417.54
Numéro MDL:
MFCD31922700
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.77

Niveau de qualité

100

Essai

≥95% (HPLC)

Forme

powder

Couleur

white to beige

Solubilité

DMSO: 2 mg/mL, clear (Wramed)

Température de stockage

2-8°C

Chaîne SMILES 

N(CCOc1ccc(cc1)\C(=C(\CCCO)/c3ccccc3)\c2ccc(cc2)O)(C)C

Clé InChI

ZVSFNBNLNLXEFQ-RQZHXJHFSA-N

Actions biochimiques/physiologiques

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).
Orally available, selective estrogen receptor-related receptor γ (ERRγ) inverse agonist with in vitro and in vivo efficacy.

Pictogrammes

Health hazard
GHS08

Mention d'avertissement

Danger

Mentions de danger

H360,H362

Classification des risques

Lact. - Repr. 1A

Code de la classe de stockage

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

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Lot/Batch Number

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Yunhui Min et al.
Pharmaceuticals (Basel, Switzerland), 13(12) (2020-12-03)
Estrogen-related receptors (ERRs) are the first identified orphan nuclear receptors. The ERR family consists of ERRα, ERRβ, and ERRγ, regulating diverse isoform-specific functions. We have reported the importance of ERRγ in osteoarthritis (OA) pathogenesis. However, therapeutic approaches with ERRγ against
Kamalakannan Radhakrishnan et al.
International journal of molecular sciences, 21(19) (2020-10-02)
Bone morphogenetic protein 6 (BMP6) is a multifunctional growth factor involved in organ development and homeostasis. BMP6 controls expression of the liver hormone, hepcidin, and thereby plays a crucial role in regulating iron homeostasis. BMP6 gene transcriptional regulation in liver
Esther Y H Chao et al.
Bioorganic & medicinal chemistry letters, 16(4), 821-824 (2005-11-26)
The design and synthesis of 4-hydroxytamoxifen (4-OHT) derivatives are described. The binding affinities of these compounds toward the orphan estrogen-related receptor gamma and the classical estrogen receptor alpha demonstrate that analogs bearing hydroxyalkyl groups display improved binding selectivity profiles compared

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