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Tibolone

Tibolone

Product ID T3305
Cas No. 5630-53-5
Purity ≥98%
Product Unit SizeCostQuantityStock
25 mg $67.80 In stock
100 mg $147.20 In stock
500 mg $338.00 In stock
1 g $525.90 In stock
Bulk Quote

Quicklinks

  • Description
  • Product Info
  • Shipping and Storage
  • Downloads
  • References
  • Description
  • Product Info
  • Shipping and Storage
  • Downloads
  • References
  • Custom Order

Description

Tibolone is a synthetic steroid hormone selective estrogen receptor modulator (SERM) that acts as an agonist or antagonist depending on the tissue location. Tibolone exhibits anti-osteoporotic, vasodilatory, and anti-metastatic activities. Tibolone has estrogenic and androgenic activity and is used for hormone replacement therapy, preventing bone loss in postmenopausal women; it acts as an agonist at progesterone and androgen receptors. Tibolone and its various metabolites act on many enzymes; they inhibit STS, 17β-HSD1, and aromatase, and activate steroid sulfotransferase and 17β-HSD2. Tibolone produces vascular relaxation in coronary arteries as well. Additionally, this compound inhibits mammary carcinoma cell invasion, likely by decreasing activity of MMP9. Tibolone is an antagonist at mineralocorticoid and glucocorticoid receptors.

Product Info

Cas No.

5630-53-5

Purity

≥98%

Formula

C21H28O2

Formula Wt.

312.45

Chemical Name

(7α,17α)-17-Hydroxy-7-methyl-19-norpregn-5(10)-en-20-yn-3-one

IUPAC Name

(7R,8R,9S,13S,14S,17R)-17-ethynyl-17-hydroxy-7,13-dimethyl-1,2,4,6,7,8, 9,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthren-3-one

Synonym

Org-OD-14, Livial

Melting Point

163-169°C

Solubility

Soluble in ethanol, DMSO, and DMF.

Appearance

White or off-white crystalline powder

Shipping and Storage

Store Temp

Ambient

Ship Temp

Ambient

Downloads

MSDS

T3305 MSDS PDF

Info Sheet

T3305 Info Sheet PDF

References

Campisi R, Marengo FD. Cardiovascular effects of tibolone: a selective tissue estrogenic activity regulator. Cardiovasc Drug Rev. 2007 Summer;25(2):132-45. PMID: 17614936.

Raobaikady B, Parsons MF, Reed MJ, et al. Tibolone and its delta-4, 7alpha-methyl norethisterone metabolite are reversible inhibitors of human aromatase. J Steroid Biochem Mol Biol. 2007 May;104(3-5):154-60. PMID: 17467267.

Vanhoecke BW, Bracke ME, Kloosterboer HJ, et al. Tibolone and its metabolites inhibit invasion of human mammary carcinoma cells in vitro. Maturitas. 2006 Jun 20;54(3):229-37. PMID: 16581209.

Lund CO, Nilas L, Pedersen SH, et al. Tibolone and its metabolites acutely relax rabbit coronary arteries in vitro. Maturitas. 2004 Nov 15;49(3):179-88. PMID: 15488346.

Kloosterboer HJ. Tissue-selectivity: the mechanism of action of tibolone. Maturitas. 2004 Aug 30;48 Suppl 1:S30-40. PMID: 15337246.

Custom Order

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