Acolbifene hydrochloride

Modify Date: 2025-08-25 13:05:34

Acolbifene hydrochloride Structure
Acolbifene hydrochloride structure
Common Name Acolbifene hydrochloride
CAS Number 252555-01-4 Molecular Weight 494.02200
Density N/A Boiling Point N/A
Molecular Formula C29H32ClNO4 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Acolbifene hydrochloride


Acolbifene (EM-652) hydrochloride, the active metabolite of EM800, is an orally active pure antiestrogen and selective estrogen receptor antagonist with an IC50 of of 0.110 nM in T-47D cells. Acolbifene (EM-652) hydrochloride possesses potent and pure anticarcinogenic properties[1][2].

 Names

Name (2S)-3-(4-hydroxyphenyl)-4-methyl-2-[4-(2-piperidin-1-ylethoxy)phenyl]-2H-chromen-7-ol,hydrochloride
Synonym More Synonyms

 Acolbifene hydrochloride Biological Activity

Description Acolbifene (EM-652) hydrochloride, the active metabolite of EM800, is an orally active pure antiestrogen and selective estrogen receptor antagonist with an IC50 of of 0.110 nM in T-47D cells. Acolbifene (EM-652) hydrochloride possesses potent and pure anticarcinogenic properties[1][2].
Related Catalog
Target

Estrogen receptor:0.110 nM (IC50, in T-47D cells.)

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 cells (ZR-75-1, MCF-7, T-47D) and is devoid of any intrinsic estrogenic activity[4].
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]. 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.
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.

[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.

[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.

[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.

 Chemical & Physical Properties

Molecular Formula C29H32ClNO4
Molecular Weight 494.02200
Exact Mass 493.20200
PSA 62.16000
LogP 6.76680
Vapour Pressure 1.42E-17mmHg at 25°C

 Synonyms

UNII-KXC7811DBY
Acolbifene hydrochloride (USAN)
Acolbifene Hydrochloride
EM 652.Hydrochloride
Acolbifene HCl
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