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Merck
모든 사진(1)

문서

SML3150

Sigma-Aldrich

GSK5182

≥95% (HPLC)

동의어(들):

(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

실험식(Hill 표기법):
C27H31NO3
CAS Number:
Molecular Weight:
417.54
MDL number:
UNSPSC 코드:
12352200
NACRES:
NA.77

Quality Level

분석

≥95% (HPLC)

형태

powder

색상

white to beige

solubility

DMSO: 2 mg/mL, clear (Wramed)

저장 온도

2-8°C

생화학적/생리학적 작용

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).

픽토그램

Health hazard

신호어

Danger

유해 및 위험 성명서

Hazard Classifications

Lact. - Repr. 1A

Storage Class Code

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

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable


시험 성적서(COA)

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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
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
Kamalakannan Radhakrishnan et al.
International journal of molecular sciences, 21(19) (2020-10-02)
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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)
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