| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| Other Sizes |
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| ln Vitro |
The cholesterol production pathway is unaffected by acobifene (ACOL), which also aids in the clearing of pertinent receptors necessary for its cholesterol-lowering action [2]. Acolbifene (EM-652) inhibits the activation of ERα and ERβ mediated by estradiol (E2) and does not exhibit any agonistic activity on ERα and ERβ transcriptional functions [3]. Acolbifene (EM-652) lacks intrinsic estrogenic activity and exhibits the strongest inhibitory impact on estradiol-stimulated cell growth in human breast cancer cells (ZR-75-1, MCF-7, and T-47D) [4].
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| ln Vivo |
In rats given a cholesterol-free diet, acolbifene (ACOL) significantly lowers cholesterolemia and decreases food intake [2]. In both diet groups, acobifene (ACOL) similarly decreased food intake (16%) and weight gain (45%, mostly fat) [2].
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| Animal Protocol |
Animal/Disease Models: Female SD (SD (Sprague-Dawley)) rats (n = 42), initial weight 175-200 g[2].
Doses: 2.5 mg/kg. Route of Administration: po (oral gavage), one time/day for 21 days. Experimental Results: Prevented tumor growth in rats. |
| References |
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| Additional Infomation |
Acolbifene Hydrochloride is the hydrochloride salt form of acolbifene, a fourth-generation estrogen receptor modulator (SERM) with potential lipid lowering and antineoplastic activity. Acolbifene specifically binds to estrogen receptors in responsive tissue, including liver, bone, breast, and endometrium. The resulting ligand-receptor complex is translocated to the nucleus where, depending on the tissue type, it promotes or suppresses the transcription of estrogen-regulated genes, thereby exerting its agonistic or antagonistic effects. Acolbifene acts as an estrogen antagonist in uterine and breast tissue, thereby blocking the effects of estrogen in these tissues. This may inhibit tumor cell proliferation in ER-positive tumor cells. This agent functions as an estrogen agonist in lipid metabolism, thereby decreasing total and LDL cholesterol levels. In bone, it decreases bone resorption and bone turnover and increases bone mineral density.
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| Molecular Formula |
C29H32CLO4
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|---|---|
| Molecular Weight |
493.03
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| Exact Mass |
493.202
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| CAS # |
252555-01-4
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| Related CAS # |
Acolbifene;182167-02-8
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| PubChem CID |
155436
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| Appearance |
White to yellow solid powder
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| Vapour Pressure |
1.42E-17mmHg at 25°C
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| LogP |
6.766
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
35
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| Complexity |
674
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC1=C([C@@H](OC2=C1C=CC(=C2)O)C3=CC=C(C=C3)OCCN4CCCCC4)C5=CC=C(C=C5)O.Cl
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| InChi Key |
BYQDPIXWTVEVEA-JMAPEOGHSA-N
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| InChi Code |
InChI=1S/C29H31NO4.ClH/c1-20-26-14-11-24(32)19-27(26)34-29(28(20)21-5-9-23(31)10-6-21)22-7-12-25(13-8-22)33-18-17-30-15-3-2-4-16-30/h5-14,19,29,31-32H,2-4,15-18H2,1H31H/t29-/m0./s1
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| Chemical Name |
2H-1-Benzopyran-7-ol, 3-(4-hydroxyphenyl)-4-methyl-2-(4-(2-(1-piperidinyl)ethoxy)phenyl)-, hydrochloride, (2S)-
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| Synonyms |
Acolbifene Hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~180 mg/mL (~364.36 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 4.5 mg/mL (9.11 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 45.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 4.5 mg/mL (9.11 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 45.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 4.5 mg/mL (9.11 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0283 mL | 10.1414 mL | 20.2827 mL | |
| 5 mM | 0.4057 mL | 2.0283 mL | 4.0565 mL | |
| 10 mM | 0.2028 mL | 1.0141 mL | 2.0283 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00853996 | Completed Has Results | Drug: acolbifene hydrochloride | Breast Cancer | University of Kansas Medical Center | February 2009 | Phase 2 |
| NCT05941520 | Not yet recruiting | Drug: Acolbifene Hydrochloride | Breast Atypical Hyperplasia Breast Carcinoma |
National Cancer Institute (NCI) | October 8, 2024 | Phase 2 |
| NCT01452373 | Completed | Drug: Placebo Drug: DHEA and Acolbifene |
Vasomotor Symptoms Hot Flushes |
EndoCeutics Inc. | October 2011 | Phase 3 |
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