Trilostane

Synonyms: WIN 24540

Trilostane (WIN 24540) is an inhibitor of 3β-hydroxysteroid dehydrogenase used in the treatment of Cushing’s syndrome.

Trilostane Chemical Structure

Trilostane Chemical Structure

CAS No. 13647-35-3

Purity & Quality Control

Trilostane Related Products

Biological Activity

Description Trilostane (WIN 24540) is an inhibitor of 3β-hydroxysteroid dehydrogenase used in the treatment of Cushing’s syndrome.
Targets
3 β-hydroxysteroid dehydrogenase [1]
In vitro
In vitro Both Trilostane and 4-Hydroxy tamoxifen (OHT) affects transcription of genes involved in cell cycle regulation, cell adhesion and matrix formation, however, only 12.5% of Trilostane down-regulated genes and 9.2% of up-regulated genes are similarly regulated by OHT in MCF-7 cells.?sup>[1]
In Vivo
In vivo Trilostane treatment results in a significant decline in basal plasma cortisol concentrations in dogs. Trilostane treatment results in an insignificant decrease in plasma aldosterone concentration (PAC), but the median plasma renin activity (PRA) at the time the trilostane dosage is considered optimal (265 fmol/L/s, range 70-3280 fmol/L/s; n=18) is significantly higher than prior to treatment (115 fmol/L/s, range 15-1330 fmol/L/s). Trilostane affects both the hypothalamic-pituitary-adrenocortical and the renin-aldosterone axes. [2] Trilostane effectively blocks the increase in systolic blood pressure and reverses the hypertension produced by drinking 0.9% saline in the Dahlsalt-sensitive rat. Trilostane is equally effective in female and male rats. [3] Trilostane reduces clinical signs and improves endocrine test results in all cats, but insulin requirements does not change and all continued to have some signs of hypercortisolemia. [4] Trilostane results in a reduction in serum cortisol and aldosteroneconcentrations in dogs with PDH, although the decrease for serum aldosterone concentration is smaller than that for serum cortisol concentration. [1]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00181597 Completed
Prostate Cancer|Prostate Adenocarcinoma
Genzyme a Sanofi Company|Sanofi
March 2004 Phase 2

Chemical Information & Solubility

Molecular Weight 329.43 Formula

C20H27NO3

CAS No. 13647-35-3 SDF Download Trilostane SDF
Smiles CC12CCC3C(C1CCC2O)CCC45C3(CC(=C(C4O5)O)C#N)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 65 mg/mL ( (197.31 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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