Estradiol sulfate
[2][4][5] Simultaneously, estrogen sulfotransferases convert estradiol to E2S, resulting in an equilibrium between the two steroids in various tissues.[11] E2S shows about 10,000-fold lower potency in activating the estrogen receptors relative to estradiol in vitro.[12] It is 10-fold less potent than estrone sulfate orally in terms of in vivo uterotrophic effect in rats.[14] This in part led to the introduction of conjugated estrogens (Premarin), which are primarily estrone sulfate, in 1941.[14] Although inactive at steroid hormone receptors, E2S has been found to act as a potent inhibitor of glutathione S-transferase,[15] an enzyme that contributes to the inactivation of estradiol via conversion of it into an estradiol-glutathione conjugate.