Tibolone

Tibolone is an estrogen-like compound used for the treatment of the symptoms associated with menopausal transition (i.e., climacteric symptoms) and also for the treatment of osteoporosis. Three major metabolites of tibolone are responsible for its tissue selective mechanism of action. Conversion into 3alpha- and 3beta-hydroxy-tibolone results in estrogenic effects in brain, vagina, and bone. The Delta4 isomer has progestrogenic and androgenic effects and does not cause estrogenic stimulation in the endometrium. A two-year longitudinal study indicates that low doses (1.25-2.5 mg) of tibolone effectively relieve climacteric symptoms and prevent loss of bone mass in early postmenopausal women.Formal Name: 17alpha-hydroxy-7alpha-methyl-19-norpregn-5(10)-en-20-yn-3-one. CAS Number: 5630-53-5. Synonyms: 7alpha-Methyl-Delta5,10-norethindrone, Org OD 14. Molecular Formula: C21H28O2. Formula Weight: 312.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMF:PBS (pH 7.2)(1:3): 0.25 mg/ml, DMSO: 20 mg/ml, Ethanol: 2 mg/ml. SMILES: O[C@@]1(C#C)CC[C@@]2([H])[C@]([C@]3([H])CC[C@@]21C)([H])[C@H](C)CC4=C3CCC(C4)=O. InChi Code: InChI=1S/C21H28O2/c1-4-21(23)10-8-18-19-13(2)11-14-12-15(22)5-6-16(14)17(19)7-9-20(18,21)3/h1,13,17-19,23H,5-12H2,2-3H3/t13-,17-,18+,19-,20+,21+/m1/s1. InChi Key: WZDGZWOAQTVYBX-XOINTXKNSA-N.