Dienogest

Dienogest is a synthetic progestin and progesterone receptor (PR) agonist (EC50s = 3.4-10.5 nM in transactivation assays). It is selective for PR over estrogen receptor alpha (ERalpha) and ERbeta, as well as glucocorticoid and mineralocorticoid receptors (EC50s = >3,000 nM for all), as well as sex hormone-binding globulin (SHBG) and cortisol-binding globulin (CBG, IC50s = 900-950 and 7,970 nM, respectively, in radioligand binding assays). It also inhibits dihydrotestosterone-induced transactivation of the androgen receptor (EC50s = 420.6-775 nM). Dienogest (0.1, 0.3, and 1 mg/kg per day for 21 days, p.o.) reduces lesion formation in a rat model of endometriosis. It reduces 17beta-estradiol benzoate-dependent tumor growth in an MCF-7 ovariectomized mouse xenograft model when administered at doses of 0.1 and 1 mg/kg per day for 28 days. Formulations containing dienogest in combination with estradiol valerate have been used as contraceptives.Formal Name: (17alpha)-17-hydroxy-3-oxo-19-norpregna-4,9-diene-21-nitrile. CAS Number: 65928-58-7. Synonyms: STS 557. Molecular Formula: C20H25NO2. Formula Weight: 311.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 2 mg/ml, DMSO: 0.1 mg/ml, Ethanol: 20 mg/ml, Ethanol:PBS (pH 7.2)(1:2): 0.3 mg/ml. lambdamax: 214, 303 nm. SMILES: O=C1CCC2=C3[C@@]([C@@](CC[C@@]4(O)CC#N)([H])[C@]4(C)CC3)([H])CCC2=C1. InChi Code: InChI=1S/C20H25NO2/c1-19-8-6-16-15-5-3-14(22)12-13(15)2-4-17(16)18(19)7-9-20(19,23)10-11-21/h12,17-18,23H,2-10H2,1H3/t17-,18+,19+,20-/m1/s1. InChi Key: AZFLJNIPTRTECV-FUMNGEBKSA-N.