MedKoo Biosciences, Inc.
Tel:   +1-919-636-5577    Fax:   +1-919-980-4831    Email:   sales@medkoo.com
Search
Login Register
Search
MedKoo Cat#: 203020 | Name: Trilostane
Featured New

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Trilostane is an inhibitor of 3β-hydroxysteroid dehydrogenase used in the treatment of Cushing's syndrome. It was withdrawn from the United States market in April 1994. However, it was recently approved in 2008 for the treatment of Cushing's disease (hyperandrenocorticism) in dogs. It is also the first drug approved to treat both pituitary- and adrenal-dependent Cushing's in dogs. This prescription drug works by stopping the production of cortisol in the adrenal glands.

Chemical Structure

Trilostane
Trilostane
CAS#13647-35-3

Theoretical Analysis

MedKoo Cat#: 203020

Name: Trilostane

CAS#: 13647-35-3

Chemical Formula: C20H27NO3

Exact Mass: 329.1991

Molecular Weight: 329.43

Elemental Analysis: C, 72.92; H, 8.26; N, 4.25; O, 14.57

Price and Availability

Size Price Availability Quantity
200mg USD 150.00 Ready to ship
500mg USD 250.00 Ready to ship
1g USD 350.00 Ready to ship
2g USD 650.00 Ready to ship
5g USD 1,250.00 Ready to ship
10g USD 1,950.00 Ready to ship
20g USD 2,950.00 Ready to ship
100g USD 4,250.00 Ready to ship
Show More
Bulk Inquiry
Buy Now
Add to Cart
Related CAS #
No Data
Synonym
WIN24540; WIN-24540; WIN 24540; Trilostane; DB01108; D-01180; D 01180; Modrastane. Desopan; Modrenal.
IUPAC/Chemical Name
(1aR,4aR,4bS,6aS,7S,9aS,9bS,11aS)-2,7-dihydroxy-4a,6a-dimethyl-1a,4,4a,4b,5,6,6a,7,8,9,9a,9b,10,11-tetradecahydrocyclopenta[7,8]phenanthro[1,10a-b]oxirene-3-carbonitrile.
InChi Key
KVJXBPDAXMEYOA-CXANFOAXSA-N
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
SMILES Code
N#CC1=C(O)[C@@]2([H])O[C@@]23[C@]([C@@]4([H])CC[C@@]5(C)[C@](CC[C@@H]5O)([H])[C@]4([H])CC3)(C)C1
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
       
Biological target:
Trilostane (Win 24540; Modrastane) is an inhibitor of 3 β-hydroxysteroid dehydrogenase.
In vitro activity:
The influence of trilostane on steroid hormone metabolism in dogs was investigated by means of an in vitro model. Canine adrenal glands from freshly euthanized dogs and corpora lutea (CL) were incubated with increasing doses of trilostane. Tritiated P5 or DHEA were used as substrates. The resulting radioactive metabolites were extracted, separated by thin layer chromatography and visualized by autoradiography. A wide variety of radioactive metabolites were formed in the adrenal glands and in the CL, indicating high metabolic activity in both tissues. In the adrenal cortex, trilostane influences the P5 metabolism in a dose- and time-dependent manner, while DHEA metabolism and metabolism of both hormones in the CL were unaffected. The results indicate for the first time that there might be more than one enzyme of 3β-HSD present in dogs and that trilostane selectively inhibits P5 conversion to P4 only in the adrenal gland. Reference: Vet Res Commun. 2012 Mar;36(1):35-40. https://link.springer.com/article/10.1007%2Fs11259-011-9509-3
In vivo activity:
The immunomodulatory effects of trilostane were examined in a contact hypersensitivity model induced by DNFB (2,4-dinitrofluorobenzene). The animals were sensitized to DNFB and then challenged on the right ear 5 days later. Ear thickness increase was used as an end point. After the initial sensitization, there was no increase in the ear thickness. On challenge 5 days later, the DNFB-challenged animals that were treated with vehicle control experienced an increase in ear thickness of 76% to 0.34 mm. The trilostane-treated animals exhibited less swelling, with a maximum thickness of 0.27 mm at 48 hours. This finding constitutes a statistically significant 19% reduction (P < 0.05) compared with the vehicle-treated group. Reference: Curr Ther Res Clin Exp. 2013 Dec;75:71-6. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3898193/
Solvent mg/mL mM
Solubility
DMSO 45.7 138.63
DMF 20.0 60.71
DMF:PBS (pH 7.2) (1:1) 0.5 1.52
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 329.43 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Ouschan C, Lepschy M, Zeugswetter F, Möstl E. 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. doi: 10.1007/s11259-011-9509-3. Epub 2011 Nov 25. PMID: 22113849. 2. Tung D, Ciallella J, Hain H, Cheung PH, Saha S. Possible therapeutic effect of trilostane in rodent models of inflammation and nociception. Curr Ther Res Clin Exp. 2013 Dec;75:71-6. doi: 10.1016/j.curtheres.2013.09.004. PMID: 24465047; PMCID: PMC3898193.
In vitro protocol:
1. Ouschan C, Lepschy M, Zeugswetter F, Möstl E. 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. doi: 10.1007/s11259-011-9509-3. Epub 2011 Nov 25. PMID: 22113849.
In vivo protocol:
1. Tung D, Ciallella J, Hain H, Cheung PH, Saha S. Possible therapeutic effect of trilostane in rodent models of inflammation and nociception. Curr Ther Res Clin Exp. 2013 Dec;75:71-6. doi: 10.1016/j.curtheres.2013.09.004. PMID: 24465047; PMCID: PMC3898193.
1: Jekl V. Adrenal Disease in Small Mammals. Vet Clin North Am Exot Anim Pract. 2025 Jan;28(1):87-106. doi: 10.1016/j.cvex.2024.07.003. Epub 2024 Oct 15. PMID: 39414475. 2: Kang HJ, Kim SW, Kim SM, La TM, Hyun JE, Lee SW, Kim JH. Altered Gut Microbiome Composition in Dogs with Hyperadrenocorticism: Key Bacterial Genera Analysis. Animals (Basel). 2024 Oct 7;14(19):2883. doi: 10.3390/ani14192883. PMID: 39409832; PMCID: PMC11476382. 3: Jiang T, Li C, Li Y, Hu W, Guo J, Du X, Meng Q, Zhu X, Song W, Guo J, Su X. Multi-omics and bioinformatics for the investigation of therapeutic mechanism of roucongrong pill against postmenopausal osteoporosis. J Ethnopharmacol. 2025 Jan 30;337(Pt 2):118873. doi: 10.1016/j.jep.2024.118873. Epub 2024 Oct 1. PMID: 39362330. 4: Furusato S, Kondo E, Tamura Y, Tsuyama Y. Successful laparotomic ethanol ablation for an adrenal tumour in a dog. Vet Med Sci. 2024 Sep;10(5):e70020. doi: 10.1002/vms3.70020. PMID: 39287218; PMCID: PMC11406512. 5: Gouvêa FN, Vargas AM, Guimarães EC, Crivellenti LZ, Pennacchi CS, de Cerqueira HDB, Branco LO, Reis NS, Borin-Crivellenti S. Association between post-ACTH cortisol and trilostane dosage in dogs with pituitary-dependent hypercortisolism. Domest Anim Endocrinol. 2024 Oct;89:106871. doi: 10.1016/j.domaniend.2024.106871. Epub 2024 Jul 4. PMID: 39032188. 6: Yun S, Yun T, Cha S, Oh J, Lee D, Koo Y, Chae Y, Yang MP, Kang BT, Kim H. Can neutrophil-to-lymphocyte and platelet-to-lymphocyte ratios be used as markers for hypercortisolism in dogs? Top Companion Anim Med. 2024 Jul-Aug;61:100890. doi: 10.1016/j.tcam.2024.100890. Epub 2024 Jul 2. PMID: 38964539. 7: Cagle LA, Casal M, Agnew D, Skinner S, Lanier CJ, Harvey JW. Atypical granulation in neutrophils of a domestic shorthair cat. Vet Clin Pathol. 2024 Jun;53(2):209-212. doi: 10.1111/vcp.13356. Epub 2024 May 26. PMID: 38797715. 8: Huang Y, Lai X, Zhang Z, Peng B, Jia X, Zou Z, Wang Y. Identification and function analysis of steroid hormone synthesis pathway-related gene-Hsd3b in Scylla paramamosain. J Steroid Biochem Mol Biol. 2024 Jul;241:106529. doi: 10.1016/j.jsbmb.2024.106529. Epub 2024 Apr 24. PMID: 38670516. 9: García San José P, Pérez-Alenza MD, Alonso-Miguel D, González Sanz S, Arenas Bermejo C. Prevalence of Systemic Hypertension and Control of Systolic Blood Pressure in a Cohort of 14 Dogs with Adrenal-Dependent Hypercortisolism during the First Year of Trilostane Treatment or after Adrenalectomy. Animals (Basel). 2024 Feb 3;14(3):511. doi: 10.3390/ani14030511. PMID: 38338154; PMCID: PMC10854962. 10: Gol M, Costa AM, Biagini G, Lucchi C. Seizure progression is slowed by enhancing neurosteroid availability in the brain of epileptic rats. Epilepsia. 2024 Mar;65(3):e41-e46. doi: 10.1111/epi.17887. Epub 2024 Jan 20. PMID: 38243753. 11: Wyatt S, Singer L, King J. Adrenocortical hemorrhage following intravenous tetracosactide in a dog with hypercortisolism. J Am Vet Med Assoc. 2023 Nov 3;262(2):1-4. doi: 10.2460/javma.23.07.0391. PMID: 37922711. 12: Tinted N, Pongcharoenwanit S, Ongvisespaibool T, Wachirodom V, Jumnansilp T, Buckland N, Chuchalermporn P, Soontararak S, Pairor S, Steiner JM, Thengchaisri N, Assawarachan SN. Serum Bile Acids Concentrations and Liver Enzyme Activities after Low-Dose Trilostane in Dogs with Hyperadrenocorticism. Animals (Basel). 2023 Oct 18;13(20):3244. doi: 10.3390/ani13203244. PMID: 37893969; PMCID: PMC10603711. 13: Park SW, Kim K, Kim OK, Ro WB, Lee CM. Case report: Successful medical management of adrenocortical carcinoma with metastasis in a Maltese dog. Front Vet Sci. 2023 Jul 14;10:1142418. doi: 10.3389/fvets.2023.1142418. PMID: 37519993; PMCID: PMC10378588. 14: Bolton TA, Panciera DL. Influence of medications on thyroid function in dogs: An update. J Vet Intern Med. 2023 Sep-Oct;37(5):1626-1640. doi: 10.1111/jvim.16823. Epub 2023 Jul 27. PMID: 37498128; PMCID: PMC10473007. 15: Erger CG, Gerras AL, Conley AJ, Gilor C, Burns DeMarle K, Refsal KR, Fleming JM, Sledge DG, Langlois DK. Case report: Androgen-secreting adrenocortical tumors in eight cats. Front Vet Sci. 2023 Jun 13;10:1158142. doi: 10.3389/fvets.2023.1158142. PMID: 37383353; PMCID: PMC10293747. 16: Hardy L, Gil-Morales C, Maunder C, Paran E. Skin fragility in a cat presenting with pituitary-dependent hyperadrenocorticism. JFMS Open Rep. 2023 Jun 20;9(1):20551169231171245. doi: 10.1177/20551169231171245. PMID: 37360386; PMCID: PMC10286191. 17: Yokota S, Kobatake Y, Maekawa M, Takashima S, Nishii N. Trismus due to myotonia associated with hyperadrenocorticism in a dog. J Vet Med Sci. 2023 Aug 1;85(8):876-879. doi: 10.1292/jvms.23-0103. Epub 2023 Jun 23. PMID: 37357395; PMCID: PMC10466053. 18: Mukangwa M, Tetsuka M. Progesterone modulates HSD11B1-mediated cortisol production in luteinized bovine granulosa cells. J Reprod Dev. 2023 Aug 11;69(4):206-213. doi: 10.1262/jrd.2023-005. Epub 2023 Jun 22. PMID: 37344443; PMCID: PMC10435524. 19: Nagata N, Aoshima K, Nakamura K, Takiguchi M. Adrenocortical hypoperfusion detected by contrast-enhanced ultrasound in a dog with trilostane-induced hypoadrenocorticism. J Small Anim Pract. 2023 Nov;64(11):722-726. doi: 10.1111/jsap.13643. Epub 2023 Jun 20. PMID: 37340686. 20: Pérez-López L, Mendoza P, Melián C. Effects of concurrent canine Cushing's syndrome and diabetes Mellitus on insulin requirements, trilostane dose, and survival time. Res Vet Sci. 2023 Aug;161:62-68. doi: 10.1016/j.rvsc.2023.06.003. Epub 2023 Jun 7. PMID: 37321012.