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SML3150

Sigma-Aldrich

GSK5182

≥95% (HPLC)

Sinónimos:

(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

Fórmula empírica (notación de Hill):
C27H31NO3
Número de CAS:
877387-37-6
Peso molecular:
417.54
MDL number:
MFCD31922700
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

100

assay

≥95% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear (Wramed)

storage temp.

2-8°C

Biochem/physiol Actions

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).

pictograms

Health hazard
GHS08

signalword

Danger

hcodes

H360,H362

Hazard Classifications

Lact. - Repr. 1A

Storage Class

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

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificados de análisis (COA)

Busque Certificados de análisis (COA) introduciendo el número de lote del producto. Los números de lote se encuentran en la etiqueta del producto después de las palabras «Lot» o «Batch»

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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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