A progestin; prodrug form of norelgestromin and levonorgestrel; binds to progestin receptors (mean IC50 = 3.48 nM for rabbit uterine receptors) and is selective for progestin over androgen receptors (mean IC50 = 764 nM for rat prostatic receptors); maintains pregnancy in ovariectomized female rats in a dose-dependent manner; inhibits ovulation in 100% of female rats at 0.5 mg/kg; completely inhibits estrone-induced vaginal cornification in ovariectomized female rats at 2 mg/kg

Norgestimate – 10 mg

Brand:
Cayman
CAS:
35189-28-7
Storage:
-20
UN-No:
Non-Hazardous - /

Norgestimate is a progestin and a prodrug form of norelgestromin and levonorgestrel (Item No. 10006318).{53982,12452} It binds to progestin receptors (mean IC50 = 3.48 nM for rabbit uterine receptors) and is selective for progestin over androgen receptors (mean IC50 = 764 nM for rat prostatic receptors) in radioligand binding assays.{53983} Norgestimate maintains pregnancy in ovariectomized female rats in a dose-dependent manner.{53982} It inhibits ovulation in 100% of female rats when administered at a dose of 0.5 mg/kg. Norgestimate (2 mg/kg) completely inhibits estrone-induced vaginal cornification in ovariectomized female rats, indicating antiestrogenic activity. Formulations containing norgestimate in combination with ethinyl estradiol have been used as oral contraceptives and in the treatment of acne vulgaris.  

 

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Description

A progestin; prodrug form of norelgestromin and levonorgestrel; binds to progestin receptors (mean IC50 = 3.48 nM for rabbit uterine receptors) and is selective for progestin over androgen receptors (mean IC50 = 764 nM for rat prostatic receptors); maintains pregnancy in ovariectomized female rats in a dose-dependent manner; inhibits ovulation in 100% of female rats at 0.5 mg/kg; completely inhibits estrone-induced vaginal cornification in ovariectomized female rats at 2 mg/kg, indicating antiestrogenic activity

Formal name: (17α)-17-(acetyloxy)-13-ethyl-18,19-dinorpregn-4-en-20-yn-3-one 3-oxime

Synonyms:  Dexnorgestrel acetime|ORF 10131

Molecular weight: 369.5

CAS: 35189-28-7

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Lipids|Sterol Lipids||Research Area|Endocrinology & Metabolism|Hormones & Receptors|Estrogens & Progestins||Research Area|Endocrinology & Metabolism|Reproductive Biology

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