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 (0-100 μM, 6 h) dose-dependently inhibits basal and gonadotrophin-stimulated small and large ovine luteal cell progesterone secretion [2]. Enclomiphene (0-100 μg/mL, 24 h) dose-dependently inhibits fertilization rates, blastocyst formation rates, and degeneration rates in mouse oocytes [3]. Enclomiphene (1 nM-10 μM, 6 h) dose-dependently decreases E2-induced inhibition of follicle stimulating hormone (FSH) secretion in primary sheep pituitary cells [4].

Enclomiphene (subcutaneous injection, 0.25 and 0.5 mg/animal, daily) inhibits spermatogenesis and decreases serum luteinizing hormone (LH) and testosterone levels in intact or castrated rats [5]. Enclomiphene (oral adminstration, 0.03-3 mg/kg, daily for 90 days) reductes body weight to sham levels, and reduced serum cholesterol [6]. Animal Model: 21 days-old Charles River male rats [5] Dosage: 0.25 and 0.5 mg/animal, daily for 24 days. Administration: Subcutaneous injection Result: Decreased LH and testosterone levels in the serum. Animal Model: OVX (ovariectomy) rat model [6] Dosage: 0.03, 1, and 3 mg/kg, daily for 90 days. Administration: Oral adminstration Result: Reducted body weight to sham levels, and reduced serum cholesterol. Showed dose-dependent effects on the proximal tibia with BMD and BMC approaching posttreatment Sham levels.