Estriol - Moligand™, 10mM in DMSO , CAS No.50-27-1

CAS: 50-27-1 Cat. No.: E408959 Fórmula: C₁₈H₂₄O₃ Peso molecular: 288.38 Beilstein Registry Number: 2508172 Número CE: 200-022-2

GRAU & PUREZA Moligand™, 10mM in DMSO

Synonyms

NSC-12169 | (16α,​17β)​-estra-​1,​3,​5(10)​-​triene-​3,​16,​17-​triol

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Visão geral

Information

Estriol (NSC-12169) is an antagonist of the G-protein coupledestrogen receptorin estrogen receptor-negative breast cancer cells.
In vitro

MTT assays using G-1 shows that, in SkBr3 cells, the proliferative effect induced by 100 nM G-1 is abolished in the presence of 1 μM estriol which acts as an antagonist of GPR30-dependent pathway. A cell-free transcription assay demonstrates that the antiestrogenic activity exhibited by estriol is because of interferring with estradiol-induced positive cooperative binding and receptor dimerization, binding of hER complexes to ERE, as well as reducing estradiol-dependent transcription in a dose-dependent manner. A recent study shows that estrogen (estrone, estradiol, and estriol) inhibits Alzheimer\'s disease-associated low-order Aβ oligomer formation, and among them, estriol shows the strongest in vitro activity.

In vivo

In mPTEN+/- mice, estriol treatments resulted in a 187.54% gain in the relative ratio of uterine wet weight to body weight; estriol also increases the ratio to 176.88% in wild-type mice. Estriol treatment (20 mg/kg ip), in vivo, sensitizes Kupffer cells to LPS via mechanisms dependent on an increase in CD14 by elevated portal blood endotoxin caused by increased gut permeability in rats; while one-half of the rats given estriol intraperitoneally 24 hours before an injection of a sublethal dose of LPS (5 mg/kg) died within 24 hours.
Cell Data

cell lines：

Concentrations：~100 nM

Incubation Time：6 days

Powder Purity:≥98%

Especificações

Sinónimos

NSC-12169 | (16α,​17β)​-estra-​1,​3,​5(10)​-​triene-​3,​16,​17-​triol

Especificações e pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos e fisiológicos

Estriol (NSC-12169) is an antagonist of the G-protein coupled estrogen receptor in estrogen receptor-negative breast cancer cells.

Condições de armazenamento de armazenamento

Store at -80°C

Enviado em

Dry ice packs + Cold packs

Este produto requer transporte de cadeia fria. Serviços terrestres e outros serviços econômicos não estão disponíveis.

Grau

Moligand™

Nomes e identificadores

SMILES isoméricas

C[C@]12CC[C@H]3[C@H]([C@@H]1C[C@H]([C@@H]2O)O)CCC4=C3C=CC(=C4)O

WGK Alemanha

3

RTECS

KG8225000

Peso molecular

288.38

Beilstein

2508172

Reaxy-Rn

2057375

Reaxys-RN_link_address

https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=2057375&ln=

Alvos associados (humanos)

ESR1 Tclin Estrogen receptor (1 Activities)

Discover Target: ESR1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ESR2 Tclin Estrogen receptor beta (1 Activities)

Discover Target: ESR2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

SHBG Tchem Sex hormone-binding globulin (0 Activities)

Discover Target: SHBG

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Propriedades químicas e físicas

• Solubilidade: Solubility (25°C) In vitro Water: 31 mg/mL (199.75 mM); DMSO: 1 mg/mL (6.44 mM); Ethanol: Insoluble
• Rotação específica [α]: 58 ° (C=0.4, Dioxane)
• Ponto de fusão (°C): 282°C