LY2066948
LY2066948 is a selective and orally active estrogen receptor modulator (SERM). LY2066948 has high affinity for estrogen receptors ERα and ERβ (Ki: 0.51 and 1.36 nM respectively) and shows potent antiestrogenic activity. LY2066948 blocks uterine weight gain induced by Ethynyl estradiol (HY-B0216) in immature rats. LY2066948 can be used for research of uterine fibroids and myomas.
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- CAS No.: 648904-56-7
- Formule: C30H31NO5S
- Masse moléculaire:517.64
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Ishikawa | IC50 |
10.7 nM
Compound: 4b
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Inhibition of estrogen stimulation in human Ishikawa cells by alkaline phosphatase quantitation
Inhibition of estrogen stimulation in human Ishikawa cells by alkaline phosphatase quantitation
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[PMID: 17482463] |
Chemical Information
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CAS No. 648904-56-7
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Masse moléculaire 517.64
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Formule C30H31NO5S
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SMILES
OC1=CC=C2C(OC3=CC=C(C=C3)OCCN4CCCCC4)=C(C=CC2=C1)C5=CC=C(C=C5)S(=O)(C)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Research Protocol for Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.
Pureté et documentation
Références
[1]. Gherezghiher TB, et al. The naphthol selective estrogen receptor modulator (SERM), LY2066948, is oxidized to an o-quinone analogous to the naphthol equine estrogen, equilenin. Chem Biol Interact. 2012 Mar 5;196(1-2):1-10. [Content Brief]
[2]. Geiser AG, et al. A new selective estrogen receptor modulator with potent uterine antagonist activity, agonist activity in bone, and minimal ovarian stimulation. Endocrinology. 2005 Oct;146(10):4524-35. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
LY2066948 Related Classifications
HY-125091 Related Classifications
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