Trilostane

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Cat Number

INT13647353

CAS Number

13647-35-3

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Product Detail Description Scientific Support Customer Q&A

CAS Number

13647-35-3

EINECS

237-133-0

Storage

2-8℃

Synonyms

(4a,5a,17b)-3,17-Dihydroxy-4,5-epoxyandrost-2-ene-2-carbonitrile;5a-Androstane-2a-carbonitrile, 4a,5-epoxy-17b-hydroxy-3-oxo-;Androst-2-ene-2-carbonitrile, 4,5-epoxy-3,17-dihydroxy-, (4a,5a,17b)-

Molecular Formula

C20H27NO3

Molecular Weight

329.43

Smiles

C[C@]12CC[C@H]3[C@H]([C@@H]1CC[C@@H]2O)CC[C@]45[C@@]3(CC(=C([C@H]4O5)O)C#N)C

Appearance

White to off-white powder

Melting Point

264℃

Boiling Point

467℃

Relative Density

1.12

pKa

8.57

General Description

Trilostane is a synthetic steroid-derived inhibitor of 3 beta-hydroxysteroid dehydrogenase (3 beta-HSD), the enzyme that catalyzes the conversion of dehydroepiandrosterone (DHEA) to androstenedione and progesterone to testosterone in the adrenal and gonadal steroidogenesis pathways. As a competitive inhibitor of 3 beta-HSD, it reduces the synthesis of androgen and estrogen steroid hormones.

Mechanism of Action

Trilostane competitively inhibits 3 beta-hydroxysteroid dehydrogenase type 2 (3 beta-HSD2), the key enzyme in the adrenal synthesis of glucocorticoids and androgens. By blocking this enzyme, trilostane reduces the production of cortisol, aldosterone, and androgens in the adrenal cortex. In Cushing's syndrome, this reduces excess cortisol production. In breast cancer, reducing systemic androgen levels decreases the substrate available for peripheral conversion to estrogen.

Application

Trilostane is indicated for the treatment of Cushing's syndrome in veterinary medicine, where it reduces excessive cortisol production. It has also been investigated in human medicine for the treatment of Cushing's syndrome, breast cancer, and conditions of androgen excess.

Trilostane is a synthetic steroid analogue that reversibly inhibits 3β-hydroxysteroid dehydrogenase (3β-HSD), blocking conversion of pregnenolone to progesterone and thereby reducing cortisol and aldosterone synthesis. It is primarily used in veterinary medicine to treat Cushing’s syndrome (hyperadrenocorticism) in dogs. Beyond endocrine disorders, trilostane increases brain levels of neurosteroids such as allopregnanolone, a positive allosteric modulator of GABAA receptors with anticonvulsant, anti-inflammatory, and anxiolytic properties. Preclinical studies in rats show that trilostane delays epileptogenesis in the kainic acid model, reduces microglial activation, and exerts analgesic effects in inflammatory pain models. It also demonstrates antidepressant- and anxiolytic-like effects in mice, associated with increased hippocampal serotonin and norepinephrine.

Fig. 1 Possible applications of Trilostane in neuronal diseases. (Olaimat A R.; et al. 2025)

References

Olaimat A R, et al. Trilostane: beyond Cushing’s syndrome. Animals, 2025, 15(3): 415.

What is the recommended storage condition for Trilostane?

It should be stored at 2-8°C in a well-sealed container, protected from moisture and direct light, to maintain its chemical integrity throughout the shelf life.

What documentation is provided with each batch of Trilostane?

Each batch is accompanied by a Certificate of Analysis (COA) covering identity, potency, and relevant purity tests. Safety Data Sheets (SDS) are available upon request.

What is the primary synthetic application of Trilostane?

It is widely used as a key building block or intermediate in multi-step pharmaceutical synthesis workflows, providing versatile reactivity for constructing target molecular architectures.

Is Trilostane compatible with common organic solvents used in pharmaceutical synthesis?

Solubility and compatibility information is available in the technical data sheet. For specific solvent compatibility questions, please contact our technical team.

What is the minimum order quantity (MOQ) for Trilostane?

Flexible MOQ options are available to support both early-stage research and large-scale manufacturing needs. Our team can tailor order quantities to match your specific requirements.