Acolbifene

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].

Product Specifications

CAS Number

[182167-02-8]

Product Name Alternative

EM-652; SCH 57068

UNSPSC

12352005

Target

Estrogen Receptor/ERR

Type

Reference compound

Related Pathways

Vitamin D Related/Nuclear Receptor

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/Acolbifene.html

Purity

99.52

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C29H31NO4

Molecular Weight

457.56

References & Citations

[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.|[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.