Clomilad (Clomiphene Citrate)

About the Product

Clomilad is a research compound from Driada Medical, containing Clomiphene Citrate. Clomiphene Citrate is a nonsteroidal, orally active agent classified as a selective estrogen receptor modulator (SERM) . Its chemical formula is C₃₂H₃₆ClNO₈, with a molecular weight of 598.09 g/mol .

The compound functions as a mixed agonist-antagonist at estrogen receptors . By binding to estrogen receptors in the hypothalamus and pituitary, it blocks the negative feedback of estradiol, leading to increased release of gonadotropin-releasing hormone (GnRH) and subsequent elevation of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) . This mechanism makes it a valuable research tool for studying the hypothalamic-pituitary-gonadal (HPG) axis.

• Product Name: Clomilad (Clomiphene Citrate)

• Brand: Driada Medical

• Form: Solution for research applications

• CAS Number: 50-41-9

• For Research Use Only.

Research Applications & Mechanism of Action

• Selective Estrogen Receptor Modulator (SERM): Clomiphene is a benchmark compound for studying estrogen receptor (ER) biology due to its tissue-specific effects . It acts as an antagonist or weak agonist depending on the target tissue, making it valuable for investigating receptor dynamics and tissue-specific signaling . Its primary action is to bind to estrogen receptors in the hypothalamus and pituitary, blocking estradiol's negative feedback and stimulating gonadotropin release .

• Hypothalamic-Pituitary-Gonadal (HPG) Axis Research: Clomiphene's ability to stimulate LH and FSH secretion makes it a key tool for studying the regulation of the HPG axis and gonadal function .

• Reproductive Research: As a stimulator of gonadotropin release, clomiphene is used in research models to study spermatogenesis, ovarian function, and fertility mechanisms .

• Endocrine Research: The compound is used to study the feedback mechanisms of estrogen and the role of estrogen receptors in the hypothalamus and pituitary .

• Comparative Studies: Clomiphene's distinct pharmacology (mixed agonist/antagonist) compared to pure antiestrogens makes it valuable for comparative studies of SERM activity .

Research & Scientific Background

• Mechanism: Clomiphene is a racemic mixture of two geometric isomers (zuclomiphene and enclomiphene) with differing activities . It binds to estrogen receptors (ERα and ERβ) in target tissues . In the hypothalamus and pituitary, the clomiphene-receptor complex blocks estradiol's negative feedback, leading to increased GnRH secretion and subsequent elevation of gonadotropin levels .

• Metabolism: The compound is extensively metabolized, primarily by cytochrome P450 enzymes (CYP3A4, CYP2D6), to active and inactive metabolites . The zuclomiphene isomer has a much longer half-life (approximately 30 days) compared to enclomiphene .

• Pharmacokinetics: Following oral administration, clomiphene has a terminal elimination half-life of approximately 5-7 days for the total drug .