Name: Trilostane
Brand: Selleck Chemicals
SKU: S1404
Rating: 5 (9 reviews)

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Quality Control

Batch: Purity: >97%

Cited in Nature Medicine for its top-tier quality
COA
Datasheet
SDS

Cited in Nature Medicine for its top-tier quality
COA
NMR
Datasheet
SDS

Cited in Nature Medicine for its top-tier quality
COA
NMR
Datasheet
SDS

97

Related Targets	HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism Drug Metabolite
Other Dehydrogenase Inhibitors	Vorasidenib (AG-881) (R)-GNE-140 CPI-613 (Devimistat) Glycyrrhizin (Glycyrrhizic Acid, NSC 167409) Sodium Dichloroacetate (DCA) AGI-5198 Gossypol Acetate AGI-6780 Emodin NCT-503

Chemical Information, Storage & Stability

Molecular Weight	329.43	Formula	C₂₀H₂₇NO₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	13647-35-3	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
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
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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
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.
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. 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. It reduces clinical signs and improves endocrine test results in all cats, but insulin requirements do not change and all continued to have some signs of hypercortisolemia. 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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/16806905/ [2] https://pubmed.ncbi.nlm.nih.gov/19042143/ [3] https://pubmed.ncbi.nlm.nih.gov/15458970/ [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

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Trilostane Dehydrogenase inhibitor

Chemical Structure

Molecular Weight: 329.43