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| Other names | NCI-122; 17β-Methyl-6,8-didehydro-17α-estradiol; 17β-Methylestra-1,3,5(10),6,8-pentaene-3,17α-diol |
| Drug class | Estrogen |
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| Chemical and physical data | |
| Formula | C19H22O2 |
| Molar mass | 282.383 g·mol−1 |
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17β-Methyl-17α-dihydroequilenin (developmental code nameNCI-122), also known as17β-methyl-6,8-didehydro-17α-estradiol, is asyntheticsteroidalestrogen which was never marketed.[1][2] It is the C17βmethylatedderivative of17α-dihydroequilenin, anequine estrogen and constituent ofconjugated estrogens (Premarin).[1][2] 17α-Dihydroequilenin itself is ananalogue of17α-estradiol, the C17epimer ofestradiol (or 17β-estradiol).[1][2] NCI-122 has respectiverelative binding affinities of about 8.1% and 16% for theERα andERβ when compared to estradiol.[2] It is far lesspotent as an estrogen in comparison to estradiol, with relative estrogenic potencies at the ERα and ERβ of 1.4% and 0.81%, respectively.[1] Nonetheless, NCI-122 acts as afull agonist of the ERα (ERβ was not assessed) and has estrogenic activity similar to that of estradiol at sufficiently high concentrations.[2] The mechanisms of the lower potency of NCI-122 and related estrogens (e.g., 17α-estradiol andequilenin) relative to estradiol have been studied.[1]
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