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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
Número MDL:
MFCD31922700
Código UNSPSC:
12352200
NACRES:
NA.77

Nivel de calidad

100

Ensayo

≥95% (HPLC)

Formulario

powder

color

white to beige

solubilidad

DMSO: 2 mg/mL, clear (Wramed)

temp. de almacenamiento

2-8°C

cadena SMILES

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

Clave InChI

ZVSFNBNLNLXEFQ-RQZHXJHFSA-N

Acciones bioquímicas o fisiológicas

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.

Pictogramas

Health hazard
GHS08

Palabra de señalización

Danger

Frases de peligro

H360,H362

Clasificaciones de peligro

Lact. - Repr. 1A

Código de clase de almacenamiento

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

Clase de riesgo para el agua (WGK)

WGK 3

Punto de inflamabilidad (°F)

Not applicable

Punto de inflamabilidad (°C)

Not applicable

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Certificados de análisis (COA)

Lot/Batch Number
0000196170
0000196171
0000189743
0000189743
0000196170

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Juhee Lim et al.
Neurochemistry international, 136, 104726-104726 (2020-03-17)
Midbrain dopaminergic (DAergic) neurotransmission plays a crucial role in regulating motor, cognitive, and emotional functions. The orphan nuclear receptor estrogen-related receptor gamma (ERRγ) is highly expressed in the adult brain and in the developing fetal brain. Our previous study showed
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
Hyo In Kim et al.
Pharmacological research, 165, 105423-105423 (2021-01-13)
Brain derived neurotrophic factor (BDNF) promotes maturation of dopaminergic (DAergic) neurons in the midbrain and positively regulates their maintenance and outgrowth. Therefore, understanding the mechanisms regulating the BDNF signaling pathway in DAergic neurons may help discover potential therapeutic strategies for
Yoon Seok Jung et al.
PloS one, 11(7), e0159425-e0159425 (2016-07-28)
Fibroblast growth factor 21 (FGF21), a stress inducible hepatokine, is synthesized in the liver and plays important roles in glucose and lipid metabolism. However, the mechanism of hepatic cannabinoid type 1 (CB1) receptor-mediated induction of FGF21 gene expression is largely
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
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