2. Vitamin D Related/Nuclear Receptor
  3. Estrogen Receptor/ERR
  4. Acolbifene

Acolbifene  (Synonyms: EM-652; SCH 57068)

Cat. No.: HY-16023A Purity: 99.52%
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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.

For research use only. We do not sell to patients.

Acolbifene Chemical Structure

Acolbifene Chemical Structure

CAS No. : 182167-02-8

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 198 In-stock
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10 mM * 1 mL in DMSO USD 198 In-stock
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1 mg USD 95 In-stock
5 mg USD 180 In-stock
10 mg USD 290 In-stock
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Based on 1 publication(s) in Google Scholar

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Acolbifene Related Antibodies

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1 Publications Citing Use of MCE Acolbifene

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Description

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[1][2][3][4][5].

IC50 & Target[5]

ERα

2 nM (IC50, E2-induced transcriptional activity)

ERβ

0.4 nM (IC50, E2-induced transcriptional activity)

In Vitro

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 Related Antibodies
In Vivo

Acolbifene (ACOL) reduces food intake and strongly decreases cholesterolemia in rats fed a cholesterol-free diet[2].
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.

Animal Model: Female Sprague-Dawley rats (n = 42) initially weighing 175-200 g[2].
Dosage: 2.5 mg/kg.
Administration: Oral gavage, once daily for 21 d.
Result: Prevents tumor growth in rats.
Clinical Trial
Molecular Weight

457.56

Formula

C29H31NO4
CAS No.
Appearance

Solid

Color

White to pink

SMILES

OC1=CC=C2C(C)=C(C3=CC=C(O)C=C3)[C@H](C4=CC=C(OCCN5CCCCC5)C=C4)OC2=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1855 mL 10.9275 mL 21.8551 mL
5 mM 0.4371 mL 2.1855 mL 4.3710 mL
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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C1

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Volume (start)

V1

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C2

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V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

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
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Acolbifene Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Acolbifene182167-02-8EM-652 SCH 57068EM652EM 652SCH57068SCH 57068SCH-57068Estrogen Receptor/ERRT-47DMCF-7MCF-7FbreastcancerERαERβZR-75-1Inhibitorinhibitorinhibit

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