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Acolbifene

CAT: 0804-HY-16023A-01Size: 1 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-16023A-01Size:1 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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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].
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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 3
Isoform
ERα; ERβ
Citation 01
Int J Mol Sci. 2022 Oct 6;23 (19) :11892.|Viruses. 2024 Aug 20;16 (8) :1332.

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