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Clomiphene, 1500mg (25mg/capsule)

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Clomiphene is a racemic mixture of two geometric isomers of a triphenylethylene selective oestrogen receptor modulator (SERM): enclomiphene (trans-isomer, predominant ER antagonist) and zuclomiphene (cis-isomer, mixed ER agonist/antagonist). The racemic mixture has a well-characterised clinical pharmacological profile as a SERM used to investigate hypothalamic–pituitary–gonadal axis feedback. Research applications include SERM pharmacology, HPG-axis feedback investigation, and isomeric mixture vs. isolated isomer comparative studies.

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3D Molecular Structure

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Chemical Formula C32H36ClNO8
Synonyms Clomiphene citrate salt, 2-(4-[2-Chloro-1,2-diphenylethenyl]phenoxy)-N,N-diethylethanamine, Clostilbegit, Dyneric, Klostilbegit, Serophene
Molar Mass 598.1 g/mol
CAS Number 50-41-9
PubChem CID 60974
Total Compound Content 1,500 mg (25 mg per capsule)
Shelf Life 36 months
Clomiphene is a synthetic triphenylethylene compound supplied as a racemic mixture of two geometric isomers: enclomiphene (~38% of mixture; trans-isomer, predominantly ER antagonist, t½ ~10 hours) and zuclomiphene (~62% of mixture; cis-isomer, mixed ER agonist-antagonist, t½ ~30 days). The combined profile — transient ER antagonism from enclomiphene plus prolonged background ER activity from zuclomiphene — produces a net increase in LH and FSH secretion via hypothalamic-pituitary ER de-repression, though the zuclomiphene accumulation complicates isomer-specific mechanistic attribution. Clomiphene has a long clinical history in reproductive endocrinology, providing extensive pharmacodynamic and safety data. It remains the reference compound for SERM-mediated HPG-axis modulation research, with enclomiphene (separate SKU) available for studies requiring isolated trans-isomer pharmacology without zuclomiphene confound. Supplied in 25 mg capsules. Independently third-party HPLC-tested; COA available per batch.

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What is the isomeric composition of clomiphene and how does it differ from enclomiphene?

Clomiphene is a racemic mixture of approximately 38% enclomiphene (trans-isomer) and 62% zuclomiphene (cis-isomer). Enclomiphene is predominantly an ER antagonist with a ~10-hour half-life. Zuclomiphene is a mixed ER agonist/antagonist with a ~30-day half-life, leading to accumulation with repeated dosing. SwissChems also supplies isolated enclomiphene (ENCLOMFNE-60) for studies requiring pure trans-isomer pharmacology without the zuclomiphene background.

Why does zuclomiphene's long half-life complicate mechanistic research with clomiphene?

Zuclomiphene accumulates with repeated dosing (t½ ~30 days vs. enclomiphene's ~10 hours), creating a progressively increasing background of ER agonist/antagonist activity that is difficult to control or quantify in repeat-dose study designs. This accumulation confounds attribution of pharmacodynamic effects to the enclomiphene component — the presumed primary active isomer for HPG-axis modulation. Researchers studying acute or isomer-specific ER antagonism at the HPG axis typically prefer isolated enclomiphene to avoid this confound.

What is clomiphene's mechanism of action at the hypothalamic-pituitary axis?

Clomiphene's primary HPG-axis mechanism is ER antagonism at hypothalamic arcuate nucleus KNDy neurons and pituitary gonadotrophs. Oestrogen-mediated negative feedback normally suppresses GnRH pulsatility and gonadotropin secretion. ER antagonism by clomiphene's enclomiphene component reduces this negative feedback, increasing GnRH pulse frequency and downstream LH/FSH secretion. The zuclomiphene component provides a counteracting partial ER agonist background that partially offsets this effect, resulting in the net gonadotropin-stimulating profile of the racemic mixture.

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