Drospirenone

Drospirenone is a synthetic progestogen that binds to the progesterone, mineralocorticoid, and androgen receptors with binding affinities of 20, 230, and 65% relative to R5020, aldosterone (Cay-15273), and R1881, respectively. In vivo, drospirenone inhibits spontaneous ovulation in rats (ID50s = 0.3-1.0 mg/day) when administered orally or subcutaneously. Drospirenone (0.5 mg/animal) administered six times per day maintains pregnancy in ovariectomized pregnant rats. It reduces serum testosterone (Cay-15645, Cay-ISO60154) and luteinizing hormone in cynomolgus monkeys in a dose-dependent manner. Drospirenone (10 mg/animal per day) also inhibits testosterone-induced growth of the seminal vesicles and prostate in castrated rats. Formulations containing drospirenone have been used as oral contraceptives.Formal Name: 1,3',4',6R,7R,8R,9S,10R,11,12,13S,14S,15S,16S,20,21-hexadecahydro-10,13-dimethyl-spiro[17H-dicyclopropa[6,7:15,16]cyclopenta[a]phenanthrene-17,2'S(5'H)-furan]-3,5'(2H)-dione. CAS Number: 67392-87-4. Synonyms: 1,2-dihydro Spirorenone, ZK 30595. Molecular Formula: C24H30O3. Formula Weight: 366.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 2 mg/ml, DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml. lambdamax: 259 nm. SMILES: O=C(CC1)O[C@@]21[C@@H](C3)[C@@H]3[C@@]4([H])[C@]5([H])[C@@H]6[C@@H](C6)C7=CC(CC[C@]7(C)[C@@]5([H])CC[C@@]42C)=O. InChi Code: InChI=1S/C24H30O3/c1-22-6-3-12(25)9-17(22)13-10-14(13)20-16(22)4-7-23(2)21(20)15-11-18(15)24(23)8-5-19(26)27-24/h9,13-16,18,20-21H,3-8,10-11H2,1-2H3/t13-,14+,15-,16+,18+,20-,21+,22-,23+,24+/m1/s1. InChi Key: METQSPRSQINEEU-HXCATZOESA-N.