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Enclomiphene (12.5mg/capsule), 60 Capsules

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Enclomiphene is the trans-geometric isomer of clomiphene, a triphenylethylene-class selective oestrogen receptor modulator (SERM). Competitive binding assays document low-nanomolar affinity for ERα and ERβ, with functional antagonism at oestrogen-responsive promoter elements in cell-based reporter models. Preclinical models utilise its HPG-axis ER-antagonist profile to investigate gonadotropin secretion dynamics and hypothalamic–pituitary feedback architecture.

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3D Molecular Structure

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Chemical Formula C26H28ClNO
Synonyms Clomiphene, Clomifene, trans-Clomiphene, Enclomifene, trans-Clomifene, Transclomifenum
Molar Mass 405.96 g/mol
CAS Number 15690-57-0
PubChem CID 1548953
Total Compound Content 750 mg (12.5 mg per capsule)
Shelf Life 36 months
Enclomiphene (trans-clomiphene) is the trans-geometric isomer of clomiphene citrate, a triphenylethylene SERM with documented high-affinity binding to ERα and ERβ (Ki low nanomolar). Unlike the cis-isomer (zuclomiphene), enclomiphene exhibits predominantly antagonist activity at oestrogen-responsive promoter elements in in vitro transcriptional reporter assays, without the mixed agonist–antagonist profile of the racemic mixture. In preclinicalmodels, systemic administration is associated with elevated LH and FSH secretion, consistent with ER antagonism at hypothalamic KNDy (kisspeptin/NKB/dynorphin) neurons and pituitary gonadotrophs. This mechanism positions enclomiphene as a precise pharmacological tool for investigating HPG-axis feedback architecture, gonadotropin pulsatility regulation, and ER-subtype selectivity in oestrogen-responsive tissues — applications where the cleaner isomeric profile offers advantages over the racemic mixture. Supplied in 12.5 mg capsules. Independently third-party HPLC-tested; COA available per batch.

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Why is enclomiphene used instead of clomiphene in HPG-axis research?

Clomiphene is a racemic mixture of enclomiphene (trans-isomer) and zuclomiphene (cis-isomer). Zuclomiphene has a plasma half-life of approximately 30 days and exhibits oestrogen-agonist activity, which confounds mechanistic studies. Enclomiphene's half-life of approximately 10 hours and clean ER-antagonist profile allow more precise investigation of HPG-axis feedback without the cumulative oestrogenic background introduced by zuclomiphene accumulation.

What is the plasma half-life of enclomiphene in preclinical models?

Enclomiphene has a plasma half-life of approximately 10 hours, with peak serum concentration reached within 2–3 hours of administration in pharmacokinetic studies. This short half-life contrasts with zuclomiphene (t½ ~30 days), preventing accumulation and enabling cleaner wash-out periods in study designs.

Which receptors does enclomiphene interact with, and how does this affect LH secretion?

Enclomiphene competitively antagonises ERα and ERβ. At the hypothalamic level, ER antagonism reduces oestrogen-mediated negative feedback on GnRH pulsatility, increasing GnRH drive to pituitary gonadotrophs and consequently elevating LH and FSH secretion. This mechanism is studied in preclinical models investigating HPG-axis feedback architecture and gonadotropin regulation.

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