Bifluranol

  Cat. No.:  DC60199   Featured
Chemical Structure
34633-34-6
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More than 5000 active chemicals with high quality for research!
Field of application
Bifluranol (brand name Prostarex; former developmental code name BX-341) is a synthetic nonsteroidal estrogen of the stilbestrol group related to diethylstilbestrol that has been used as an antiandrogen in the United Kingdom in the treatment of benign prostatic hyperplasia. It exerts functional antiandrogen effects by binding to and activating the estrogen receptor in the pituitary gland, consequently suppressing the secretion of luteinizing hormone (and hence acting as an antigonadotropin) and thereby reducing gonadal androgen production and systemic androgen levels.
Cas No.: 34633-34-6
Chemical Name: Phenol,4,4'-[(1R,2S)-1-ethyl-2-methyl-1,2-ethanediyl]bis[2-fluoro-, rel-
SMILES: CCC(C1=CC(F)=C(O)C=C1)C(C)C2=CC(F)=C(O)C=C2
Formula: C17H18O2F2
M.Wt: 292.32042
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: BX341 is an anti-androgen.
Target: Androgen Receptor[1]
In Vivo: The absorption, distribution and excretion of BX341 (Bifluranol) have been studied in mouse, rat, ferret and dog; BX341is readily absorbed following oral administration, but blood concentrations of BX341 are low due to hepatic uptake and biliary excretion. After intravenous administration of [3H] BX341 to rats (200 μg/kg) and ferrets (60 μg/kg) the blood concentrations of 3H decreases rapidly for the first 2 to 3 h, with the decrease being more rapid in females ( 18 min for rat, 30 min for ferret) than males (1.0 h for rat, 1.4 h for ferret). This is followed by a much slower decline (40 h for rat, 20 h for ferret) to concentrations at 96 h of less than 15 ng BX341 equivalents mL-1 (rat) or 1 ng BX341 equivalents mL-1 (ferret)[1].
In Vitro: Mice, Rats, Dogs and Ferrets[1] Swiss albino mice (24-28 g, males age 4 weeks, females age 6 weeks; pregnant mice mated at 6 weeks, used at day 18 of pregnancy) and Wistar albino rats (200 g males age 6 weeks, females age 8 weeks; 350 g males age 10 weeks) are fed Dixon's mouse and rat diet and have free access to water. Albino ferrets (0.7-2.6 kg, age 9-15 months) are fed raw meat, bread and milk. Male beagles (10.8-12.3 kg, age 10-14 years) are fed Spratt's complete dog diet. [3H] BX341 administration is by intragastric intubation, in propylene glycol (mouse 0.1 ml, rat 0.1-0.2 mL, ferret 0.1-0.4 mL and dog 1 mL), except for the dog 96 h excretion study when the drug is absorbed onto starch and given in a gelatin capsule. BX341 is given intravenously in propylene glycol-0.9% NaCl (saline) (1 : 1 v/v) (0.1-0.2 mL), via a tail vein in mice and rats and the jugular vein in ferrets (under ether anaesthesia). [3H] BX341 (2 mg/kg, 1.1 mCi) is administered orally or intravenously to male, female and pregnant mice. After various time intervals they are killed under ether anaesthesia by immersion in solid CO2-hexane (-70°C). The tail, limbs and ears are removed. The animals shaved, embedded and frozen in 5 % aq. acacia wax. The animal blocks are cut using a Slee whole-body freezing microtome to obtain lateral sections (30 pm) which are exposed to X-ray film at 4°C and the auto-radiograms examined after 1,3 or 6 months. [3H]Bifluranol is adrninistered orally or intravenously to rats (200 μg/kg, 0.86-1.0 mCi) , ferrets (60 μg/kg, 5.0-10.6 mCi) and orally only to dogs (50 μg/kg, 70-76 mCi) . Blood samples (10-100 μL) are taken for radioactivity determination at time intervals up to 96 h (rat and ferret) or 6 h (dog).
References: [1]. Pope DJ, et al. Bifluranol, a novel fluorinated bibenzyl anti-androgen, its chemistry and disposition in different animal species. J Pharm Pharmacol. 1981 May;33(5):297-301.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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