Acolbifene
Based on 2 publication(s) in Google Scholar
Acolbifene (EM-652), the active metabolite of EM800, is an orally active pure antiestrogen and selective estrogen receptor antagonist. Acolbifene (EM-652) inhibits estradiol (E2)-induced transcriptional activity of ERα (IC50 = 2 nM) and ERβ (IC50 = 0.4 nM). Acolbifene (EM-652) possesses potent and pure anticarcinogenic properties.
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- 純度: 99.42%
- CAS 番号: 182167-02-8
- 分子式: C29H31NO4
- 分子量:457.56
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 Acolbifene
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生物活性
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ERα 2 nM (IC50, E2-induced transcriptional activity) |
ERβ 0.4 nM (IC50, E2-induced transcriptional activity) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| ZR-75-1 | IC50 |
0.55 nM
Compound: (S)-6 (EM-652)
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Inhibition of estradiol-stimulated ZR-75-1-cell proliferation
Inhibition of estradiol-stimulated ZR-75-1-cell proliferation
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[PMID: 9216828] |
Acolbifene (ACOL) does not affect pathways of cholesterol synthesis, supporting the involvement of the clearance-related receptors in its hypocholesterolemic action[2].
Acolbifene (EM-652) shows no agonistic activity on ERα and ERβ transcriptional function and blocks the estradiol (E2)-mediated activation of both ERα and ERβ[3].
Acolbifene (EM-652) shows the most potent inhibition of estradiol-stimulated cell proliferation in human breast cancer cancer cells (ZR-75-1, MCF-7, T-47D) and is devoid of any intrinsic estrogenic activity[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Acolbifene (ACOL) reduces food intake (16%) and weight gain (45%, mainly fat) similarly in both dietary cohorts[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female Sprague-Dawley rats (n = 42) initially weighing 175-200 g[2].
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Dosage:2.5 mg/kg.
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Administration:Oral gavage, once daily for 21 d.
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Result:Prevents tumor growth in rats.
化学情報
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CAS 番号 182167-02-8
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性状 Solid
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分子量 457.56
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分子式 C29H31NO4
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Color White to pink
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SMILES
OC1=CC=C2C(C)=C(C3=CC=C(O)C=C3)[C@H](C4=CC=C(OCCN5CCCCC5)C=C4)OC2=C1
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別名
EM-652; SCH 57068
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Int J Mol Sci
Identification of Candidate Genes in Breast Cancer Induced by Estrogen Plus Progestogens Using Bioinformatic Analysis. [Abstract]2022 Oct 6;23(19):11892. PMID: 36233194 -
Viruses
Antiviral Activity of Selective Estrogen Receptor Modulators against Severe Fever with Thrombocytopenia Syndrome Virus In Vitro and In Vivo. [Abstract]2024 Aug 20;16(8):1332. PMID: 39205306
溶剤 & 溶解度
DMSO : 50 mg/mL (109.28 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (275 KB)
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SDS (251 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Wang T, et al. Recent advances in selective estrogen receptor modulators for breast cancer. Mini Rev Med Chem. 2009 Sep;9(10):1191-201. [Content Brief]
[2]. Christian Lemieux, et al. The selective estrogen receptor modulator acolbifene reduces cholesterolemia independently of its anorectic action in control and cholesterol-fed rats. J Nutr. 2005 Sep;135(9):2225-9. [Content Brief]
[3]. A Tremblay, et al. EM-800, a novel antiestrogen, acts as a pure antagonist of the transcriptional functions of estrogen receptors alpha and beta. Endocrinology. 1998 Jan;139(1):111-8. [Content Brief]
[4]. Sylvain Gauthier, et al. Synthesis and structure-activity relationships of analogs of EM-652 (acolbifene), a pure selective estrogen receptor modulator. Study of nitrogen substitution. J Enzyme Inhib Med Chem. 2005 Apr;20(2):165-77. [Content Brief]
[5]. F Labrie, et al. EM-652 (SCH 57068), a third generation SERM acting as pure antiestrogen in the mammary gland and endometrium. J Steroid Biochem Mol Biol. Apr-Jun 1999;69(1-6):51-84. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1855 mL | 10.9275 mL | 21.8551 mL | 54.6376 mL |
| 5 mM | 0.4371 mL | 2.1855 mL | 4.3710 mL | 10.9275 mL | |
| 10 mM | 0.2186 mL | 1.0928 mL | 2.1855 mL | 5.4638 mL | |
| 15 mM | 0.1457 mL | 0.7285 mL | 1.4570 mL | 3.6425 mL | |
| 20 mM | 0.1093 mL | 0.5464 mL | 1.0928 mL | 2.7319 mL | |
| 25 mM | 0.0874 mL | 0.4371 mL | 0.8742 mL | 2.1855 mL | |
| 30 mM | 0.0729 mL | 0.3643 mL | 0.7285 mL | 1.8213 mL | |
| 40 mM | 0.0546 mL | 0.2732 mL | 0.5464 mL | 1.3659 mL | |
| 50 mM | 0.0437 mL | 0.2186 mL | 0.4371 mL | 1.0928 mL | |
| 60 mM | 0.0364 mL | 0.1821 mL | 0.3643 mL | 0.9106 mL | |
| 80 mM | 0.0273 mL | 0.1366 mL | 0.2732 mL | 0.6830 mL | |
| 100 mM | 0.0219 mL | 0.1093 mL | 0.2186 mL | 0.5464 mL |
Acolbifene 関連分類
HY-16023A 関連分類
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