Ospemifene

Ospemifene (FC-1271a) is an orally active and non-estrogenic selective estrogen receptor modulator (SERM) with Ki values of 380 and 410 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene inhibits caspase-3 activity. Ospemifene inhibits neuronal degeneration, prevents bone loss, and increases vaginal weight and vaginal epithelial height. Ospemifene has anticancer activity against breast cancer[1][2][3][4][5][6].

Product Specifications

CAS Number

[128607-22-7]

Product Name Alternative

FC-1271a

UNSPSC

12352005

Hazard Statement

H410

Target

Caspase; Estrogen Receptor/ERR

Type

Reference compound

Related Pathways

Apoptosis; Vitamin D Related/Nuclear Receptor

Applications

Cancer-programmed cell death

Field of Research

Cancer; Endocrinology; Neurological Disease

Assay Protocol

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

Purity

99.84

Solubility

DMSO : ≥ 100 mg/mL

Smiles

ClCC/C(C1=CC=CC=C1)=C(C2=CC=C(OCCO)C=C2)\C3=CC=CC=C3

Molecular Formula

C24H23ClO2

Molecular Weight

378.89

Precautions

H410

References & Citations

[1]Qiang Qv.et al.Selective estrogenic effects of a novel triphenylethylene compound, FC1271a, on bone, cholesterol level, and reproductive tissues in intact and ovariectomized rats. Endocrinology.Feb;141 (2) :809-20. 25. (2000) .|[2]Tracy L. Taras et al.In vitro and in vivo biologic effects of Ospemifene (FC-1271a) in breast cancer. The Journal of Steroid Biochemistry and Molecular Biology 77 (4-5) :271-9, (2001) .|[3]Unkila M, et, al. Vaginal effects of ospemifene in the ovariectomized rat preclinical model of menopause. J Steroid Biochem Mol Biol. 2013 Nov;138:107-15.|[4]Bruyniks N, et, al. Systematic indirect comparison of ospemifene versus local estrogens for vulvar and vaginal atrophy. Climacteric. 2017 Jun; 20 (3) : 195-204.|[5]Pietrzak B A, et al. Posttreatment with ospemifene attenuates hypoxia-and ischemia-induced apoptosis in primary neuronal cells via selective modulation of estrogen receptors. Neurotoxicity Research, 2023, 41 (4) : 362-379.|[6]Burich RA, et al. Ospemifene and 4-hydroxyospemifene effectively prevent and treat breast cancer in the MTag.Tg transgenic mouse model. Menopause. 2012 Jan;19 (1) :96-103.