Chlorotrianisene (trade name Tace) is a non-steroidal synthetic estrogen that was formerly used for the treatment of menopause, deficiencies in ovary function, and prostate cancer. Chlorotrianisene (TACE) may react vigorously with strong oxidizing agents. Can react exothermically with reducing agents (such as alkali metals and hydrides) to release gaseous hydrogen. May react exothermically with both acids and bases. TAM and TACE exhibit protein-specific estrogen agonist and antagonist efficacies in lactotrophs, with the estrogen induction of glandular kallikrein being particularly sensitive to antagonism by TAM in vivo. Chlorotrianisene (TACE) exhibits in vitro little or no binding to the uterine estrogen receptor (ER) but demonstrates potent estrogenic activity in vivo, indicating that TACE is a proestrogen/proantiestrogen. Chlorotrianisene could inhibit bone loss and delay the atrophy of uterus induced by ovariectomy in Wistar female rats. It has protective effects on bone like other estrogen preparations.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Prevention of bone loss by chlorotrianisene in oophorectomized rats.
Zhang J, et al. Zhonghua Fu Chan Ke Za Zhi. 1997 Sep;32(9):535-7. PMID: 9639753.
Monooxygenase-mediated activation of chlorotrianisene (TACE) in covalent binding to rat hepatic microsomal proteins.
Juedes MJ, et al. Drug Metab Dispos. 1987 Nov-Dec;15(6):786-93. PMID: 2893703.
Differential responses of pituitary kallikrein and prolactin to tamoxifen and chlorotrianisene.
Powers CA, et al. Mol Cell Endocrinol. 1989 Sep;66(1):93-100. PMID: 2583366.
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.
Kupfer D, et al. FEBS Lett. 1990 Feb 12;261(1):59-62. PMID: 2307235.
|Related Estrogen Receptor Products|
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Elagolix Soidum is a potent, selective, orally active, non-peptide antagonist of the gonadotropin-releasing hormone receptor (GnRHR) with Kd value of 54 pM.
GDC-0810 (Brilanestrant, ARN-81) is an orally bioavailable selective estrogen receptor degrader (SERD) with IC50 of 0.7 nM.
Tamoxifen is a estrogen receptor partial agonist/antagonist.
GSK 4716 is a selective agonist with estrogen-related receptors ERRβ and ERRγ.
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