Acolbifene hydrochloride
Based on 2 publication(s) in Google Scholar
Acolbifene (EM-652) hydrochloride, an active metabolite of EM800, is an orally active, cancer-preventing selective estrogen receptor modulator (SERM). Acolbifene (EM-652) hydrochloride inhibits estradiol (E2)-induced transcriptional activity of ERα (IC50=2 nM) and ERβ (IC50=0.4 nM). Acolbifene (EM-652) hydrochloride exerts a potent and pure antiestrogenic action in the mammary gland and uterus. Anticarcinogenic properties.
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- Reinheit: 99.00%
- CAS. Nr.: 252555-01-4
- Formel: C29H32ClNO4
- Molecular Weight:494.02
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Acolbifene hydrochloride
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Biologische Aktivität
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ERα 2 nM (IC50, E2-induced transcriptional activity) |
ERβ 0.4 nM (IC50, E2-induced transcriptional activity) |
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 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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 252555-01-4
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Appearance Solid
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Molecular Weight 494.02
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Formel C29H32ClNO4
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Color White to yellow
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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.[H]Cl
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Synonyms
EM-652 hydrochloride; SCH 57068 hydrochloride
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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
Lösungsmittel & Löslichkeit
DMSO : 180 mg/mL (364.36 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 4.5 mg/mL (9.11 mM); Clear solution
This protocol yields a clear solution of ≥ 4.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (45.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 4.5 mg/mL (9.11 mM); Clear solution
This protocol yields a clear solution of ≥ 4.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (45.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
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Data Sheet (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
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- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[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 (sealed storage, away from moisture). 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 |
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| DMSO | 1 mM | 2.0242 mL | 10.1210 mL | 20.2421 mL | 50.6052 mL |
| 5 mM | 0.4048 mL | 2.0242 mL | 4.0484 mL | 10.1210 mL | |
| 10 mM | 0.2024 mL | 1.0121 mL | 2.0242 mL | 5.0605 mL | |
| 15 mM | 0.1349 mL | 0.6747 mL | 1.3495 mL | 3.3737 mL | |
| 20 mM | 0.1012 mL | 0.5061 mL | 1.0121 mL | 2.5303 mL | |
| 25 mM | 0.0810 mL | 0.4048 mL | 0.8097 mL | 2.0242 mL | |
| 30 mM | 0.0675 mL | 0.3374 mL | 0.6747 mL | 1.6868 mL | |
| 40 mM | 0.0506 mL | 0.2530 mL | 0.5061 mL | 1.2651 mL | |
| 50 mM | 0.0405 mL | 0.2024 mL | 0.4048 mL | 1.0121 mL | |
| 60 mM | 0.0337 mL | 0.1687 mL | 0.3374 mL | 0.8434 mL | |
| 80 mM | 0.0253 mL | 0.1265 mL | 0.2530 mL | 0.6326 mL | |
| 100 mM | 0.0202 mL | 0.1012 mL | 0.2024 mL | 0.5061 mL |
Acolbifene hydrochloride Related Classifications
HY-16023 Related Classifications
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