Enclomiphene citrate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Enclomiphene citrate((E)-Clomifene、cis-Clomifene、RMI-16289、ICI-46476) 是一种非甾体选择性雌激素受体调节剂 (SERM)。

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.

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.

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.

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

Endocrinology/Hormones

Estrogen Receptor/ERR

Estrogen Receptor/ERR

Endocrinology

Sexual Dysfunction

7599-79-3

598.089

C32H36ClNO8

>98% (HPLC)

10 mM in DMSO

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

(E)-2-(4-(2-chloro-1,2-diphenylvinyl)phenoxy)-N,N-diethylethan-1-amine 2-hydroxypropane-1,2,3-tricarboxylate

(-20℃)

With Ice Pack

≥ 2 years