Norgestimate

Norgestimate is a progestin and a prodrug form of norelgestromin and levonorgestrel (Cay-10006318). 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. Norgestimate maintains pregnancy in ovariectomized female rats in a dose-dependent manner. 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.Formal Name: (17alpha)-17-(acetyloxy)-13-ethyl-18,19-dinorpregn-4-en-20-yn-3-one 3-oxime. CAS Number: 35189-28-7. Synonyms: Dexnorgestrel acetime, ORF 10131, RWJ 10131. Molecular Formula: C23H31NO3. Formula Weight: 369.5. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 16 mg/ml, DMF:PBS(pH7.2) (1:2): 0.3 mg/ml, DMSO: 14 mg/ml, Ethanol: 2 mg/ml. lambdamax: 241 nm. SMILES: CC[C@@]12[C@](CC[C@@]2(OC(C)=O)C#C)([H])[C@]3([H])CCC4=C/C(CC[C@]4([H])[C@@]3([H])CC1)=N/O. InChi Code: InChI=1S/C23H31NO3/c1-4-22-12-10-19-18-9-7-17(24-26)14-16(18)6-8-20(19)21(22)11-13-23(22,5-2)27-15(3)25/h2,14,18-21,26H,4,6-13H2,1,3H3/b24-17+/t18-,19+,20+,21-,22-,23-/m0/s1. InChi Key: KIQQMECNKUGGKA-NMYWJIRASA-N.