| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| Other Sizes |
Purity: ≥98%
| Targets |
Bifluranol targets the estrogen receptor (ER) and indirectly modulates the androgen axis. By activating estrogen receptors in the pituitary, it suppresses luteinizing hormone (LH) secretion, thereby acting as an antigonadotropin and reducing gonadal androgen production and systemic androgen levels. It is also described as having anti-androgenic activity.
|
|---|---|
| ln Vitro |
In vitro, Bifluranol binds to and activates estrogen receptors, demonstrating non-steroidal estrogenic activity. The compound's ability to activate estrogen receptors in the pituitary is the basis for its functional anti-androgenic effects. Its activity has been characterized in receptor binding and functional assays.
|
| ln Vivo |
Diflunol's distribution, absorption, and excretion have all been studied in mice, rats, ferrets, and dogs. Although diflunol is easily absorbed when taken orally, its concentration in blood is lower because of hepatic absorption and bile excretion. Following an intravenous injection of [3H]difluorol in rats (200 μg/kg) and ferrets (60 μg/kg), there was a rapid decrease in 3H blood concentrations within the first two to three hours. In female mice, this decrease was more rapid (18 minutes). compared to males (rats 1.0 hours, ferrets 1.4 hours) (rats, 30 minutes). Following this, the concentration drops below 15 ng bisfluranol equivalent mL-1 (rat) or 1 ng bisfluranol equivalent mL-1 (ferret) after 96 hours, with the rate of decline being much slower (40 hours for rats and 20 hours for ferrets) [1].
In vivo, Bifluranol has shown significant anti-prostatic activity in preclinical studies for the treatment of benign prostatic hyperplasia (BPH). The compound has been evaluated in animal models including rat, ferret, and dog following oral administration. Its functional anti-androgenic effects reduce androgen-driven prostate growth. |
| Enzyme Assay |
For receptor binding assays, Bifluranol is incubated with estrogen receptors from pituitary tissue or recombinant ER proteins. Competitive binding studies using radiolabeled estradiol are performed to determine binding affinity. Functional assays measure the compound's ability to activate estrogen-responsive reporter gene expression in transfected cells.
|
| Cell Assay |
Cellular assays utilize cell lines expressing estrogen receptors or pituitary-derived cells. Cells are treated with Bifluranol at various concentrations and assessed for estrogen-responsive gene expression using luciferase reporter assays or qPCR. The compound's ability to modulate gonadotropin-releasing hormone receptor signaling may also be evaluated.
|
| Animal Protocol |
In vivo studies are conducted in rat, ferret, and dog models. Bifluranol is administered orally, and endpoints include assessment of prostate weight, serum androgen levels, and LH concentrations. The compound's anti-prostatic activity is evaluated in models of androgen-dependent prostate growth such as BPH or prostate cancer xenografts.
|
| ADME/Pharmacokinetics |
Bifluranol (molecular weight 292.32) is a small-molecule nonsteroidal estrogen with good oral bioavailability. Following oral administration, it shows systemic exposure and tissue distribution consistent with its mechanism of action. The compound has been evaluated in multiple species including rat, ferret, and dog.
|
| Toxicity/Toxicokinetics |
Preclinical toxicology studies have evaluated Bifluranol in animal models. As a compound with estrogenic activity, its toxicity profile includes effects related to hormonal modulation. The compound has been studied for BPH with a focus on its safety and tolerability. No significant toxicity has been reported at therapeutic doses.
|
| References | |
| Additional Infomation |
(2S,3R)-Difluorool is a 4,4'-pentane-2,3-dimethylbis(2-fluorophenol) with a (2S,3R)-stereoconfiguration. It is the enantiomer of (2R,3S)-difluorool.
Bifluranol (BX341) is a synthetic nonsteroidal compound that was investigated for the treatment of benign prostatic hyperplasia (BPH). Its mechanism involves activation of estrogen receptors in the pituitary, leading to suppression of LH secretion and reduction of gonadal androgen production. Despite promising preclinical activity, Bifluranol never progressed to clinical use and today serves primarily as a reference compound for probing androgen receptor pathways and evaluating next-generation antiandrogen therapeutics. |
| Molecular Formula |
C17H18O2F2
|
|---|---|
| Molecular Weight |
292.32042
|
| Exact Mass |
292.127
|
| CAS # |
34633-34-6
|
| PubChem CID |
12850912
|
| Appearance |
White to off-white solid powder
|
| Density |
1.221g/cm3
|
| Boiling Point |
361.6ºC at 760mmHg
|
| Flash Point |
172.5ºC
|
| Index of Refraction |
1.565
|
| LogP |
4.673
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
21
|
| Complexity |
326
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
CC[C@@H](C1=CC(=C(C=C1)O)F)[C@H](C)C2=CC(=C(C=C2)O)F
|
| InChi Key |
RDVXUHOSYIBGBT-ZWNOBZJWSA-N
|
| InChi Code |
InChI=1S/C17H18F2O2/c1-3-13(12-5-7-17(21)15(19)9-12)10(2)11-4-6-16(20)14(18)8-11/h4-10,13,20-21H,3H2,1-2H3/t10-,13-/m1/s1
|
| Chemical Name |
Phenol, 4,4'-(1-ethyl-2-methyl-1,2-ethanediyl)bis(2-fluoro-, (R*,S*)-
|
| Synonyms |
BX-341; BX-341; BX-341; traded name Prostarex
|
| HS Tariff Code |
2934.99.9001
|
| 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 (~342.09 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.55 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.55 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 | 3.4209 mL | 17.1045 mL | 34.2091 mL | |
| 5 mM | 0.6842 mL | 3.4209 mL | 6.8418 mL | |
| 10 mM | 0.3421 mL | 1.7105 mL | 3.4209 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