Home Metabolism Dehydrogenase inhibitor Trilostane

research use only

Trilostane Dehydrogenase inhibitor

Cat.No.S1404

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

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Chemical Information, Storage & Stability

Molecular Weight 329.43 Formula

C20H27NO3

 Storage (From the date of receipt)
CAS No. 13647-35-3 Download SDF Storage of Stock Solutions

Synonyms WIN 24540 Smiles CC12CCC3C(C1CCC2O)CCC45C3(CC(=C(C4O5)O)C#N)C

Solubility

In vitro
Batch:

DMSO : 65 mg/mL (197.31 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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

mg/kg
g
μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO
%
% Tween 80
% ddH2O
% DMSO
+
%

Calculation results:

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.

Mechanism of Action

Targets/IC50/Ki
3 β-hydroxysteroid dehydrogenase [1]
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
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]
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/15478772/
  • [5] https://pubmed.ncbi.nlm.nih.gov/15478772/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00181597 Completed
Prostate Cancer|Prostate Adenocarcinoma
Genzyme a Sanofi Company|Sanofi
 March 2004 Phase 2

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Signaling Pathway Map