product name Ethinyl Estradiol
Description: Ethinyl Estradiol is an orally bio-active estrogen used in almost all modern formulations of combined oral contraceptive pills. It is a synthetic analog of estradiol commonly used as an oral contraceptive, often in combination with a progestin. Efficacy of oral administration is facilitated by the ethynyl substitution at the C-17 position, which inhibits first pass hepatic metabolism. It is rapidly absorbed from gastrointestinal tract.
References: Toxicol Sci. 1999;51(2):224-35; Toxicol Sci. 2003;75(2):271-8. 2003; Toxicol Sci. 2010;114(1):133-48.
296.4
Formula
C20H24O2
CAS No.
57-63-6
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 59 mg/mL (199.1 mM)
Water: <1 mg/mL
Ethanol: 59 mg/mL (199.1 mM)
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19417858
| In Vitro |
In vitro activity: Ethinyl Estradiol increases respiratory chain activity in both cultured rat hepatocytesand HepG2 cells. Ethinyl estradiol is a strong promoter of hepatocarcinogenesis. Ethinyl Estradiol enhances the transcript levels of nuclear genome- and mitochondrial genome-encoded genes and respiratory chain activity in female rat liver, and also inhibits transforming growth factor beta (TGFbeta)-induced apoptosis in cultured liver slices and hepatocytes from female rats. Ethinyl Estradiol increases the transcript levels of the mitochondrial genome-encoded genes cytochrome oxidase subunits I, II, and III in cultured female rathepatocytes. Ethinyl Estradiol significantly increases both the levels of glutathione (reduced [GSH] and oxidized [GSSG] forms) per mg protein in mitochondria and nuclei, while the percentage of total glutathione in the oxidized form is not affected. Kinase Assay: Cell Assay: |
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| In Vivo | Ethinyl Estradiol (50 mg/kg/day) increases anogenital distance and reduces pup body weight at postnatal day 2, accelerates the age at vaginal opening, reduces F1 fertility and F2 litter sizes, and induces malformations of the external genitalia (5 mg/kg) in the female Long-Evans rat. Ethinyl Estradiol increases the number of low density lipoprotein (LDL) receptors in livers of rats, thereby producing a profound fall in plasma cholesterol levels. Ethinyl Estradiol exerts the same effect in livers of male and female rabbits and that the increase in receptor number is correlated with a 6- to 8-fold increase in the levels of receptor mRNA. |
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| References | Toxicol Sci. 1999 Oct;51(2):224-35; Toxicol Sci. 2003 Oct;75(2):271-8. Epub 2003 Jul 11; Toxicol Sci. 2010 Mar;114(1):133-48. |
