Acolbifene (Synonyms: EM-652; SCH 57068)

Name: Acolbifene
Brand: MedChemExpress
SKU: HY-16023A
Rating: 5.0 (2 reviews)

Cat. No.: HY-16023A Purity: 99.52%: FAQs
Data Sheet SDS COA Handling Instructions

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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

CAS No. : 182167-02-8

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 198	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 198	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 95	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 180	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 290	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Acolbifene:

(Rac)-Acolbifene Get quote
Acolbifene hydrochloride Get quote

2 Publications Citing Use of MCE Acolbifene

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View All Estrogen Receptor/ERR Isoform Specific Products:

View All Isoforms

Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

Biological Activity
Purity & Documentation
References
Customer Review

Description

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.

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.

182167-02-8

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
10 mM	0.2186 mL	1.0928 mL	2.1855 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

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(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

Purity: 99.52%

Select Batch:

Data Sheet (274 KB) SDS (251 KB)

COA (247 KB) LCMS (96 KB)

Handling Instructions (2659 KB)

References

[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

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 Related Classifications

Cancer

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.

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Acolbifene (Synonyms: EM-652; SCH 57068)

Customer Review

Other Forms of Acolbifene:

Acolbifene Related Antibodies

2 Publications Citing Use of MCE Acolbifene

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Estrogen Receptor/ERR Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Acolbifene Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Acolbifene Related Classifications

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