Enclomiphene citrate

SKU: orb1224054

Description

Enclomiphene citrate((E)-Clomifene, cis-Clomifene, RMI-16289, ICI-46476) is a nonsteroidal selective estrogen receptor modulator (SERM) that is under development for the treatment of male hypogonadism; inhibits the ER in the pituitary gland, reduces negative feedback by estrogen on the hypothalamic-pituitary-gonadal axis, increases gonadotropin secretion and hence gonadal production of testosterone.Sexual Dysfunction Phase 3 Clinical(In Vitro):Enclomiphene citrate (0-100 μM, 6 h) dose-dependently inhibits basal and gonadotrophin-stimulated small and large ovine luteal cell progesterone secretion.Enclomiphene citrate (0-100 μg/mL, 24 h) dose-dependently inhibits fertilization rates, blastocyst formation rates, and degeneration rates in mouse oocytes.Enclomiphene citrate (1 nM-10 μM, 6 h) dose-dependently decreases E2-induced inhibition of follicle stimulating hormone (FSH) secretion in primary sheep pituitary cells.(In Vivo):Enclomiphene citrate (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.Enclomiphene citrate (oral adminstration, 0.03-3 mg/kg, daily for 90 days) reductes body weight to sham levels, and reduced serum cholesterol.

Key Properties

• CAS Number: 7599-79-3
• MW: 598.089
• Purity: >98% (HPLC)
• Formula: C₃₂H₃₆ClNO₈
• SMILES: CCN(CC)CCOC1=CC=C(C=C1)C(=C(C2=CC=CC=C2)Cl)C3=CC=CC=C3.C(C(=O)O)C(CC(=O)O)(C(=O)O)O
• Target: Estrogen Receptor/ERR
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  Enclomiphene citrate (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. Enclomiphene citrate (oral adminstration, 0.03-3 mg/kg, daily for 90 days) reductes body weight to sham levels, and reduced serum cholesterol. Animal model: 21 days-old Charles River male rats. 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. 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.
• In Vitro:
  Enclomiphene citrate (0-100 μM, 6 h) dose-dependently inhibits basal and gonadotrophin-stimulated small and large ovine luteal cell progesterone secretion. Enclomiphene citrate (0-100 μg/mL, 24 h) dose-dependently inhibits fertilization rates, blastocyst formation rates, and degeneration rates in mouse oocytes. Enclomiphene citrate (1 nM-10 μM, 6 h) dose-dependently decreases E2-induced inhibition of follicle stimulating hormone (FSH) secretion in primary sheep pituitary cells.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

E)-Clomifene | cis-Clomifene | RMI-16289 | ICI-46476

Quick Database Links

Gene Symbol

Estrogen Receptor/ERR