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Tibolone

Cat. No. M21213
Tibolone Structure
Synonym:

Org OD 14;Org OD14

Size Price Availability Quantity
100mg USD 400  USD400 In stock
500mg USD 900  USD900 In stock
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Quality Control & Documentation
Biological Activity

Tibolone is a synthetic anabolic steroid with estrogenic, androgenic and progestagenic activities. The 3alpha- and 3beta-hydroxy metabolites of tibilone activate estrogenic receptors (ERs) in bone and vaginal tissue leading to a decrease in bone turnover, and decreased vaginal dryness, respectively; derived from the 3beta-hydroxy metabolite, its delta4-isomer activates androgenic receptors (ARs) in the brain and liver and progestogenic receptors (PRs) in endometrial tissue, affecting sexual function, lipid metabolism, and endometrial function, respectively. In breast and endometrial tissue, tibolone metabolites inhibit sulfatase, preventing the conversion of circulating estrone sulfate and estradiol sulfate to estrone and estradiol, respectively; estrogen-mediated effects in the breast and uterus are thus reduced.

Chemical Information
Molecular Weight 312.45
Formula C21H28O2
CAS Number 5630-53-5
Solubility (25°C) N/A
Storage RT
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Qi Yuan, et al. Steroids. Does tibolone treatment have favorable effects on obesity, blood pressure, and inflammation? A meta-analysis of randomized controlled trials

[2] Juan Pablo Del Ro, et al. Trends Endocrinol Metab. Tibolone as Hormonal Therapy and Neuroprotective Agent

[3] Giulio Formoso, et al. Cochrane Database Syst Rev. Short-term and long-term effects of tibolone in postmenopausal women

[4] P Albertazzi, et al. Maturitas. Tibolone: a review

[5] L A Ross, et al. Maturitas. Tibolone and climacteric symptoms

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Keywords: Tibolone, Org OD 14;Org OD14 supplier, Estrogen Receptor, inhibitors, activators


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