| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| 1g |
|
||
| Other Sizes |
|
Purity: ≥98%
Chlorotrianisene is a long-acting, orally bioactive non-steroidal synthetic estrogen that was used for the treatment of menopause, deficiencies in ovary function, and prostate cancer.
| ln Vitro |
Initial evidence of the potential for ER activation as a growth-stimulating mechanism is provided by comparing the intracellular estrogen receptor (ER) affinity of chlortrianisene with the comparable rat uterine cytosolic ER affinity. With a 500 nM Ki and an EC50 of 28 nM, chlorotrianisene stimulates cell proliferation in MCF-7 cells in a concentration-dependent manner[1].
|
|---|---|
| ln Vivo |
Rat liver microsomes and NADPH were incubated with chlortrianisene to produce reaction intermediates that covalently bound to the protein. The uterine estrogen receptor may be rendered inactive by intermediates (ER). Under conditions that resulted in intermediates, the ER binding capacity for [3H]estradiol (E2) was significantly reduced when chlorotrianisene was incubated with rat liver microsomes and NADPH in the presence of a rat uterus [3].
|
| References |
[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. |
| Molecular Formula |
C23H21CLO3
|
|---|---|
| Molecular Weight |
380.86
|
| Exact Mass |
380.11792
|
| CAS # |
569-57-3
|
| Related CAS # |
Chlorotrianisene-d9;1276197-26-2
|
| SMILES |
COC1=CC=C(C=C1)C(=C(C2=CC=C(C=C2)OC)Cl)C3=CC=C(C=C3)OC
|
| InChi Key |
BFPSDSIWYFKGBC-UHFFFAOYSA-N InChi Code
|
| Chemical Name |
1-[1-chloro-2,2-bis(4-methoxyphenyl)ethenyl]-4-methoxybenzene
|
| Synonyms |
Chlorotrianisene Chlortrianisestrol Chlortrianizen Chlorotrianisine Chlorestrolo Chlorotrianizen Khlortrianizen Clorestrolo Clorotrisin Hormonisene Anisene Metace Rianil Tace
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~262.56 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.56 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.56 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6256 mL | 13.1282 mL | 26.2564 mL | |
| 5 mM | 0.5251 mL | 2.6256 mL | 5.2513 mL | |
| 10 mM | 0.2626 mL | 1.3128 mL | 2.6256 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA