product name Mestranol
Description: Mestranol is the 3-methyl ether of ethinyl estradiol, which is a potent estrogen receptor agonist and used as oral contraceptives. Mestranol is the 3-methyl ether of ethinylestradiol. It is a biologically inactive prodrug of ethinylestradiol to which it is demethylated in the liver with a conversion efficiency of 70% (50 μg of mestranol is pharmacokinetically bioequivalent to 35 μg of ethinylestradiol).
References: Carcinogenesis. 1996 Sep;17(9):2043-52; Brain Res Bull. 1988 Aug;21(2):329-33.
310.43
Formula
C21H26O2
CAS No.
72-33-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 15 mg/mL (48.3 mM)
Water: <1 mg/mL
Ethanol: 25 mg/mL (80.5 mM)
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19418012
| In Vitro |
In vitro activity: Mestranol is extensively metabolized to hydroxylated products whose bio- logical activity is less well characterized. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Mestranol (0.2 mg/kg) results in an increased percentage of liver occupied by AHF expressing glutathione S-transferase (PGST) in rats. Mestranol administration increases the focal hepatocyte labeling index compared with the control with a trend at the lower dose and a significant difference at the higher dose. Mestranol (0.02 mg/kg and 0.2 mg/kg diet) results in a decrease in the non-focal labeling index compared with that observed for the corresponding concentration of Mestranol alone. Mestranol significantly increases the non-focal hepatic labeling index in uninitiated rats compared with that observed in rats administered the basal diet only. Mestranol (50 mg/100 g b.wt.) has a significant reduction in the apparent number of alpha-2-adrenoceptors in the frontal cortex and nucleus tractus solitarius (NTS) of rat, while apparent numbers of both alpha-1 and alpha-2-adrenoceptors are depressed in the locus coeruleus. |
| Animal model | |
| Formulation & Dosage | |
| References | Carcinogenesis. 1996 Sep;17(9):2043-52; Brain Res Bull. 1988 Aug;21(2):329-33. |
