Acolbifene (hydrochloride)

$180$1,200

Products Details

Product Description

– Acolbifene (EM-652) hydrochloride, an active metabolite of EM800, is an orally active, cancer-preventing selective estrogen receptor modulator (SERM). Acolbifene (EM-652) hydrochloride inhibits estradiol (E2)-induced transcriptional activity of ERα (IC50=2 nM) and ERβ (IC50=0.4 nM). Acolbifene (EM-652) hydrochloride exerts a potent and pure antiestrogenic action in the mammary gland and uterus. Anticarcinogenic properties[1][2][3][4][5].

Web ID

– HY-16023

Storage Temperature

– 4°C (Powder, sealed storage, away from moisture)

Shipping

– Room Temperature

Applications

– Cancer-programmed cell death

Molecular Formula

– C29H32ClNO4

References

– [1]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.|[2]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.|[3]Wang T, et al. Recent advances in selective estrogen receptor modulators for breast cancer. Mini Rev Med Chem. 2009 Sep;9(10):1191-201.|[4]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.|[5]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.

CAS Number

– 252555-01-4

Molecular Weight

– 494.02

Compound Purity

– 99.00

SMILES

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

Clinical Information

– Phase 3

Research Area

– Cancer

Solubility

– DMSO : 180 mg/mL (ultrasonic)

Target

– Estrogen Receptor/ERR

Isoform

– ERα;ERβ

Pathway

– Vitamin D Related/Nuclear Receptor

Product type

– Reference compound

Disclaimer: All products are for Research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation. Agdia Products are available for delivery only in Canada.

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