Droloxifene

Droloxifene, a Tamoxifen derivative, is an orally active and selective estrogen receptor modulator. Droloxifene shows antiestrogenic and anti-implantation effects. Droloxifene induces p53 expression and apoptosis in MCF-7 cells. Droloxifene prevents bone loss in ovariectomized rats.

Product information

CAS Number: 82413-20-5

Molecular Weight: 387.51

Formula: C26H29NO2

Synonym:

3-Hydroxytamoxifen

Chemical Name: 3-[(1E)-1-{4-[2-(dimethylamino)ethoxy]phenyl}-2-phenylbut-1-en-1-yl]phenol

Smiles: CC/C(=C(\C1=CC(O)=CC=C1)/C1C=CC(=CC=1)OCCN(C)C)/C1C=CC=CC=1

InChiKey: ZQZFYGIXNQKOAV-OCEACIFDSA-N

InChi: InChI=1S/C26H29NO2/c1-4-25(20-9-6-5-7-10-20)26(22-11-8-12-23(28)19-22)21-13-15-24(16-14-21)29-18-17-27(2)3/h5-16,19,28H,4,17-18H2,1-3H3/b26-25+

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

Droloxifene (10 nM; 16-18 hours) induces apoptosis in MCF-7 cells.

In Vivo:

Droloxifene (5-20 mg/kg; p.o.; daily for 4 weeks) increases BMD of DFM at 10mg/kg, and completely prevents the decrease of BMC and BMD of DFM induced by ovariectomized (OVX) at 20 mg/kg/day.

References:

1. Herrington DM, et al. Cardiovascular effects of droloxifene, a new selective estrogen receptor modulator, in healthypostmenopausal women. Arterioscler Thromb Vasc Biol. 2000 Jun;20(6):1606-12.
2. Grasser WA, et al. Common mechanism for the estrogen agonist and antagonist activities of droloxifene. J Cell Biochem. 1997 May;65(2):159-71.
3. Ke HZ, et al. Droloxifene, a new estrogen antagonist/agonist, prevents bone loss in ovariectomized rats. ndocrinology. 1995 Jun;136(6):2435-41.

Products are for research use only. Not for human use.