| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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Purity: ≥98%
Trilostane (also known as WIN 24540; Desopan; DB-011080; Win-24540; Modrastane) is a potent inhibitor of 3β-hydroxysteroid dehydrogenase that was used in the treatment of Cushing's syndrome, Conn's syndrome, and postmenopausal breast cancer in humans. However, Trilostane was withdrawn from the United States in the 1990s and was later approved as a veterinary medicine for use in the treatment of Cushing's syndrome in dogs.
| ln Vitro |
Adrenocortical pregnenolone metabolism is impacted by trilostane in a time- and dose-dependent way [2]. Trilostane specifically prevents the adrenal gland from converting pregnenolone to progesterone [2].
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| ln Vivo |
Dogs with pituitary-dependent elevated adrenocortical hormone levels are managed with trimostane (5.3–50 mg/kg; PO once daily for three months) [1].
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| Animal Protocol |
Animal/Disease Models: Dogs with naturally-occurring pituitary-dependent hyperadrenocorticism (PDH)[1]
Doses: 5.3-50 mg/kg Route of Administration: Oral administration; 5.3-50 mg/kg, one time/day for 3 months Experimental Results: Effectively achieved endocrine control with safe effects and free of side-effects. |
| ADME/Pharmacokinetics |
Metabolism / Metabolites
Hepatic. Biological Half-Life 8 hours. |
| References |
[1]. JA Braddock, et al. Trilostane treatment in dogs with pituitary-dependent hyperadreno-corticism. Veterinary Journal. 10 March 2008.
[2]. Ouschan C, et al. The influence of trilostane on steroid hormone metabolism in canine adrenal glands and corpora lutea-an in vitro study. Vet Res Commun. 2012 Mar;36(1):35-40. |
| Additional Infomation |
Trilostane can cause developmental toxicity according to state or federal government labeling requirements.
Trilostane is an epoxy steroid that is 3,17beta-dihydroxy-5alpha-androst-2-ene-2-carbonitrile in which the oxygen of the epoxy group is joined to the 4alpha and 5 alpha positions. It has a role as an antineoplastic agent, an abortifacient and an EC 1.1.1.210 [3beta(or 20alpha)-hydroxysteroid dehydrogenase] inhibitor. It is a 3-hydroxy steroid, a 17beta-hydroxy steroid, an androstanoid, an epoxy steroid and a nitrile. Trilostane is an inhibitor of 3 beta-hydroxysteroid dehydrogenase used in the treatment of Cushing's syndrome. It was withdrawn from the United States market in April 1994. Trilostane is a synthetic derivative of androstane with adrenocortical suppressive properties. Trilostane reversibly inhibits 3 beta-hydroxysteroid dehydrogenase delta 5-4 isomerase in the adrenal cortex, resulting in the decreased synthesis of mineralocorticoids and glucocorticoids and the decreased conversion of pregnenolone to progesterone. (NCI04) Drug Indication Used in the treatment of Cushing's syndrome. It is normally used in short-term treatment until permanent therapy is possible. Mechanism of Action Trilostane produces suppression of the adrenal cortex by inhibiting enzymatic conversion of steroids by 3-beta-hydroxysteroid dehydrogenase/delta 5,4 ketosteroid isomerase, thus blocking synthesis of adrenal steroids. |
| Molecular Formula |
C20H27NO3
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| Molecular Weight |
329.43
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| Exact Mass |
329.199
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| CAS # |
13647-35-3
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| Related CAS # |
Trilostane-d3
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| PubChem CID |
656583
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
497.8±45.0 °C at 760 mmHg
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| Melting Point |
264ºC
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| Flash Point |
254.8±28.7 °C
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| Vapour Pressure |
0.0±2.9 mmHg at 25°C
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| Index of Refraction |
1.610
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| LogP |
3.61
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
24
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| Complexity |
692
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| Defined Atom Stereocenter Count |
8
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| SMILES |
O1[C@]2([H])C(=C(C#N)C([H])([H])[C@]3(C([H])([H])[H])[C@@]4([H])C([H])([H])C([H])([H])[C@]5(C([H])([H])[H])[C@]([H])(C([H])([H])C([H])([H])[C@@]5([H])[C@]4([H])C([H])([H])C([H])([H])[C@]132)O[H])O[H]
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| InChi Key |
KVJXBPDAXMEYOA-CXANFOAXSA-N
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| InChi Code |
InChI=1S/C20H27NO3/c1-18-7-6-14-12(13(18)3-4-15(18)22)5-8-20-17(24-20)16(23)11(10-21)9-19(14,20)2/h12-15,17,22-23H,3-9H2,1-2H3/t12-,13-,14-,15-,17+,18-,19+,20+/m0/s1
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| Chemical Name |
(1S,2R,6R,8S,11S,12S,15S,16S)-5,15-dihydroxy-2,16-dimethyl-7-oxapentacyclo[9.7.0.02,8.06,8.012,16]octadec-4-ene-4-carbonitrile
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (7.59 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (7.59 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.59 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0355 mL | 15.1777 mL | 30.3555 mL | |
| 5 mM | 0.6071 mL | 3.0355 mL | 6.0711 mL | |
| 10 mM | 0.3036 mL | 1.5178 mL | 3.0355 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00181597 | Completed | Drug: Trilostane Drug: Hydrocortisone |
Prostate Cancer Prostate Adenocarcinoma |
Genzyme, a Sanofi Company | March 2004 | Phase 2 |
| NCT01615211 | Terminated | Drug: Letrozole Drug: Trilostane |
Medical Abortion, Complete or Unspecified, Without Complication |
Kristina Gemzell Danielsson | May 2012 | Phase 2 |
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