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| Formula | C20H24O4 |
| Molar mass | 328.408 g·mol−1 |
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16α-LE2, or16α-lactone-estradiol, also known as3,17β-dihydroxy-19-nor-17α-pregna-1,3,5-(10)-triene-21,16α-lactone, is asynthetic,steroidalestrogen featuring anestradiol core. It is a highly potent and selectiveagonist of theERα that is used inscientific research to study the function of the ERα.[1][2] It has 265-fold higherpotency intransactivationassays of the ERα relative to theERβ and 70-fold preference inbinding affinity for the ERα over the ERβ.[2]
In rodents, 16α-LE2 has no effect onovarian follicle development, whereas the highly ERβ-selective agonist8β-VE2 stimulates follicular growth and to a comparable extent asestradiol, indicating that the ERβ and not the ERα is involved in the effects of estrogen on ovarian follicles.[2][3] In contrast, 16α-LE2 stimulatesuterine weight, whereas 8β-VE2 has no effect, indicating that the ERα and not the ERβ is involved in the effects of estrogen on the uterus.[2] Research has determined through experimentalrodent studies with estradiol, 16α-LE2, and 8β-VE2 that the positive, protective effects of estrogens onbone formationresorption andbone mineral density are mediated via the ERα, whereas the ERβ does not appear to be involved.[4]
