1、BX341Cat. No.: HY-U00229CAS No.: 34633-34-6Molecular Formula: CHFOMolecular Weight: 292.32Target: Androgen ReceptorPathway: OthersStorage: Please store the product under the recommended conditions in the COA.Solvent BX341is readily absorbed following oral administration, but blood concentrations of
2、BX341 are low due to hepatic uptake and biliary excretion. After intravenous administration of 3H BX341 to rats (200 g/kg) and ferrets (60 g/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)
3、 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.PROTOCOLProduct Data Sheet InhibitorsAgonistsScreening Libraries
4、www.MedChemE1Animal Administration 1Mice, Rats, Dogs and Ferrets1 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 D
5、ixons 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 Spratts complete dog diet. 3H BX341 administration is by intragastric intubation, in propylene glycol (mouse 0.1
6、 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 j
7、ugular 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 (-70C). The tail, limbs and ears are removed.
8、 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 4C and the auto-radiograms examined after 1,3 or 6 months. 3HBifluranol is adrninistered orally o
9、r intravenously to rats (200 g/kg, 0.86-1.0 mCi) , ferrets (60 g/kg, 5.0-10.6 mCi) and orally only to dogs (50 g/kg, 70-76 mCi) . Blood samples (10-100 L) are taken for radioactivity determination at time intervals up to 96 h (rat and ferret) or 6 h (dog). MCE has not independently confirmed the acc
10、uracy of these methods. They are for reference only.REFERENCES1. 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.Caution: Product has not been fully validated for medical applications. For research use only.Tel: 609-228-6898 Fax: 609-228-5909 E-mail: techMedChemEAddress: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USAwww.MedChemE2
