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Chlorotrianisene

Cat. No. M3692
Chlorotrianisene Structure
Synonym:

Chlortrianizen, Chlorotrianisine

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
50mg USD 40  USD40 In stock
100mg USD 70  USD70 In stock
500mg USD 210  USD210 In stock
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Quality Control & Documentation
Biological Activity

Chlorotrianisene is a non-steroidal synthetic estrogen that was formerly used for the treatment of menopause, deficiencies in ovary function, and prostate cancer. Chlorotrianisene may react vigorously with strong oxidizing agents. Can react exothermically with reducing agents (such as alkali metals and hydrides) to release gaseous hydrogen. Chlorotrianisene exhibits in vitro little or no binding to the uterine estrogen receptor (ER) but demonstrates potent estrogenic activity in vivo, indicating that Chlorotrianisene 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.

Chemical Information
Molecular Weight 380.86
Formula C23H21ClO3
CAS Number 569-57-3
Solubility (25°C) DMSO ≥ 50 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Zhang J, et al. Zhonghua Fu Chan Ke Za Zhi. Prevention of bone loss by chlorotrianisene in oophorectomized rats.

[2] Juedes MJ, et al. Drug Metab Dispos. Monooxygenase-mediated activation of chlorotrianisene (TACE) in covalent binding to rat hepatic microsomal proteins.

[3] Powers CA, et al. Mol Cell Endocrinol. Differential responses of pituitary kallikrein and prolactin to tamoxifen and chlorotrianisene.

[4] Kupfer D, et al. FEBS Lett. 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.

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Keywords: Chlorotrianisene, Chlortrianizen, Chlorotrianisine supplier, Estrogen Receptor, inhibitors, activators


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