Home Metabolism Dehydrogenase inhibitor Trilostane

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Trilostane Dehydrogenase inhibitor

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

Trilostane Dehydrogenase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 329.43

Purity & Quality Control

Related Products

Signaling Pathway

Dehydrogenase Signaling Pathways

Dehydrogenase Signaling Pathway

Mechanism of Action

Targets
3 β-hydroxysteroid dehydrogenase [1]

In vitro
In vitro Both Trilostane and 4-Hydroxy tamoxifen (OHT) affect transcription of genes involved in cell cycle regulation, cell adhesion and matrix formation, however, only 12.5% of this compound down-regulated genes and 9.2% of up-regulated genes are similarly regulated by OHT in MCF-7 cells.[1]

In Vivo
In vivo Trilostane treatment results in a significant decline in basal plasma cortisol concentrations in dogs. This compound 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). It affects both the hypothalamic-pituitary-adrenocortical and the renin-aldosterone axes. [2] This compound effectively blocks the increase in systolic blood pressure and reverses the hypertension produced by drinking 0.9% saline in the Dahlsalt-sensitive rat. It is equally effective in female and male rats. [3] It 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] It results in a reduction in serum cortisol and aldosterone concentrations 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

References
  • https://pubmed.ncbi.nlm.nih.gov/16806905/
  • https://pubmed.ncbi.nlm.nih.gov/19042143/
  • https://pubmed.ncbi.nlm.nih.gov/15458970/
  • https://pubmed.ncbi.nlm.nih.gov/15478772/
  • https://pubmed.ncbi.nlm.nih.gov/15478772/

Chemical Information

Molecular Weight 329.43 Formula

C20H27NO3
CAS No. 13647-35-3 SDF Download SDF
Synonyms WIN 24540
Smiles CC12CCC3C(C1CCC2O)CCC45C3(CC(=C(C4O5)O)C#N)C

Storage and Stability

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


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

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In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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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