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Merck

PZ0183

Sigma-Aldrich

ERB-041

≥98% (HPLC)

Synonym(e):

2-(3-Fluoro-4-hydroxyphenyl)-7-vinyl-1,3-benzoxazol-5-ol, Prinaberel, WAY-202041

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About This Item

Empirische Formel (Hill-System):
C15H10FNO3
CAS-Nummer:
Molekulargewicht:
271.24
MDL-Nummer:
UNSPSC-Code:
51111800
PubChem Substanz-ID:
NACRES:
NA.77

Assay

≥98% (HPLC)

Form

powder

Farbe

white to tan

Löslichkeit

DMSO: ≥25 mg/mL

Lagertemp.

room temp

SMILES String

OC(C=C1)=C(F)C=C1C2=NC3=CC(O)=CC(C=C)=C3O2

InChI

1S/C15H10FNO3/c1-2-8-5-10(18)7-12-14(8)20-15(17-12)9-3-4-13(19)11(16)6-9/h2-7,18-19H,1H2

InChIKey

MQIMZDXIAHJKQP-UHFFFAOYSA-N

Angaben zum Gen

human ... ESR2(2100)

Biochem./physiol. Wirkung

ERB-041 is a potent, selective ERβ receptor agonist (IC50 ERβ: 5.4 nM; > 200-fold selective over ERα)
ERB-041 is a potent, selective estrogen ERβ receptor agonist (IC50 ERβ: 5.4 nM; > 200-fold selective over ERα). ERβ plays a minor role in mediating estrogen action in the uterus, the hypothalamus/pituitary, the skeleton, and other classic estrogen target tissues. However, a clear role for ERβ has been established in the ovary, cardiovascular system, and brain as well as in animal models of inflammation including arthritis, endometriosis, inflammatory bowel disease, and sepsis. There is increasing interest in finding ERβ agonists for potential use in a variety of clinical applications without triggering classic estrogenic side effects.

Leistungsmerkmale und Vorteile

This compound is featured on the Nuclear Receptors (Steroids) page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Piktogramme

Exclamation mark

Signalwort

Warning

H-Sätze

Gefahreneinstufungen

Acute Tox. 4 Oral - Eye Irrit. 2

Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 3

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable


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Die Dokumentenbibliothek aufrufen

Qian Jiang et al.
Purinergic signalling, 13(1), 105-117 (2016-11-07)
Estrogen receptor beta (ERβ) has been shown to play a therapeutic role in inflammatory bowel disease (IBD). However, the mechanism underlying how ERβ exerts therapeutic effects and its relationship with P2X3 receptors (P2X3R) in rats with inflammation is not known.
Iuliia Savchuk et al.
PloS one, 8(8), e71722-e71722 (2013-08-24)
It is well known that estrogens and estrogen-like endocrine disruptors can suppress steroidogenic gene expression, attenuate androgen production and decrease differentiation of adult Leydig cell lineage. However, there is no information about the possible link between the potency of Leydig
Sreenivasan Paruthiyil et al.
PloS one, 4(7), e6271-e6271 (2009-07-18)
Estrogens produce biological effects by interacting with two estrogen receptors, ERalpha and ERbeta. Drugs that selectively target ERalpha or ERbeta might be safer for conditions that have been traditionally treated with non-selective estrogens. Several synthetic and natural ERbeta-selective compounds have
Lili Zhang et al.
PloS one, 5(7), e11791-e11791 (2010-07-30)
Estrogens are used extensively to treat hot flashes in menopausal women. Some of the beneficial effects of estrogens in hormone therapy on the brain might be due to nongenomic effects in neurons such as the rapid stimulation of calcium oscillations.
Ana Paola G Lombardi et al.
Frontiers in endocrinology, 11, 184-184 (2020-04-25)
Prostate cancer is initially dependent on the androgen, gradually evolves into an androgen-independent form of the disease, also known as castration-resistant prostate cancer (CRPC). At this stage, current therapies scantily improve survival of the patient. Androgens and estrogens are involved

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