Enclomiphene ((E)-Clomiphene) is a potent and orally active antagonist of non-steroidal estrogen receptor. Enclomiphene has research value in ovarian dysfunction, testosterone deficiency, male hypogonadism and type 2 diabetes.

Enclomiphene administrated in a dose-dependent manner (0-100 μM, 6 h) reduces both basal and gonadotrophin-stimulated progesterone secretion in small and large ovine luteal cells, as well as inhibiting fertilization, blastocyst formation, and oocyte degeneration rates in mice when applied at 0-100 μg/mL for 24 h. Additionally, enclomiphene (1 nM-10 μM, 6 h) counteracts the E2-induced suppression of follicle-stimulating hormone (FSH) secretion in primary sheep pituitary cells, showcasing its varying pharmacological effects across different biological systems and conditions.

Enclomiphene, administered via subcutaneous injection at dosages of 0.25 and 0.5 mg/animal daily, inhibits spermatogenesis and decreases serum luteinizing hormone (LH) and testosterone levels in both intact and castrated Charles River male rats aged 21 days, after 24 days of treatment. Similarly, oral administration of Enclomiphene at dosages ranging from 0.03 to 3 mg/kg daily for 90 days in an ovariectomy (OVX) rat model results in a reduction of body weight to sham levels, decreased serum cholesterol, and demonstrates dose-dependent improvements in bone mineral density (BMD) and bone mineral content (BMC) in the proximal tibia, approaching post-treatment sham levels.