| Bioactivity | Chlorotrianisene is a long-acting non-steroidal estrogen and an orally active estrogen receptor modulator. Chlorotrianisene exhibits antiestrogenic activity. Chlorotrianisene potently inhibits the enzyme COX-1 and inhibits platelet aggregation in whole blood[1][2][3]. | ||||||||||||
| Target | Estrogen receptorCOX-1 | ||||||||||||
| Invitro | Comparison of intracellular estrogen receptor (ER) affinities of Chlorotrianisene with respective rat uterine cytosolic ER affinities has initially suggested the potential for activation of ER as a mechanism of growth stimulation. Chlorotrianisene exhibits concentration dependent cell growth stimulation with an EC50 of 28 nM and a Ki of 500 nM in MCF-7 cells[1]. | ||||||||||||
| In Vivo | The incubation of Chlorotrianisene with rat liver microsomes and NADPH generates a reactive intermediate which binds covalently to proteins. Intermediate may inactivate the uterine estrogen receptors (ER). The incubation of Chlorotrianisene with rat liver microsomes and NADPH in the presence of rat uteri, under conditions which generate intermediate, markedly decreased the binding capacity of the ER for [3H]estradiol (E2)[3]. | ||||||||||||
| Name | Chlorotrianisene | ||||||||||||
| CAS | 569-57-3 | ||||||||||||
| Formula | C23H21ClO3 | ||||||||||||
| Molar Mass | 380.86 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Ruenitz PC, et al. Estrogenic tamoxifen derivatives: categorization of intrinsic estrogenicity in MCF-7 cells. J Steroid Biochem Mol Biol. 1997 Nov-Dec;63(4-6):203-9. [2]. Lounkine E, et al. Large-scale prediction and testing of drug activity on side-effect targets. Nature. 2012 Jun 10;486(7403):361-7. [3]. Kupfer D, et al. Inactivation of the uterine estrogen receptor binding of estradiol during P-450 catalyzed metabolism of chlorotrianisene (TACE). Speculation that TACE antiestrogenic activity involves covalent binding to the estrogen receptor. FEBS Lett. |
Chlorotrianisene
CAS: 569-57-3 F: C23H21ClO3 W: 380.86
Chlorotrianisene is a long-acting non-steroidal estrogen and an orally active estrogen receptor modulator. Chlorotrianis
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