A tissue-selective steroid with estrogenic and androgenic effects
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Tibolone

Item No. 10006321

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
17α-hydroxy-7α-methyl-19-norpregn-5(10)-en-20-yn-3-one
CAS Number
5630-53-5
Synonyms
  • 7α-Methyl-Δ5,10-norethindrone
  • Org OD 14
Molecular Formula
C21H28O2
Formula Weight
312.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS (pH 7.2)(1:3): 0.25 mg/mlDMSO: 20 mg/mlEthanol: 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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    100 mg

    $38

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    250 mg

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    500 mg

    $168

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    1 g

    $316

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    Product Description

    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.1 Three major metabolites of tibolone are responsible for its tissue selective mechanism of action. Conversion into 3α- and 3β-hydroxy-tibolone results in estrogenic effects in brain, vagina, and bone. The Δ4 isomer has progestrogenic and androgenic effects and does not cause estrogenic stimulation in the endometrium.1 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.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kloosterboer, H.J. Tissue-selectivity: The mechanism of action of tibolone. Maturitas 48(Suppl 1), S30-S40 (2004).

    2. Gambacciani, M., Ciaponi, M., Cappagli, B., et al. A longitudinal evaluation of the effect of two doses of tibolone on bone density and metabolism in postmenopausal women. Gynecol. Endocrinol. 18(1), 9-16 (2004).