Trilostane

Catalog No.S1404 Batch:S140401

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Technical Data

Formula

C20H27NO3
Molecular Weight 329.43 CAS No. 13647-35-3
Solubility (25°C)* In vitro DMSO 66 mg/mL (200.34 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
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.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Trilostane (WIN 24540) is an inhibitor of 3β-hydroxysteroid dehydrogenase used in the treatment of Cushing’s syndrome.
Targets
3 β-hydroxysteroid dehydrogenase [1]
In vitro Both Trilostane and 4-Hydroxy tamoxifen (OHT) affects transcription of genes involved in cell cycle regulation, cell adhesion and matrix formation, however, only 12.5% of Trilostane down-regulated genes and 9.2% of up-regulated genes are similarly regulated by OHT in MCF-7 cells.?sup>[1]
In vivo Trilostane treatment results in a significant decline in basal plasma cortisol concentrations in dogs. Trilostane 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). Trilostane affects both the hypothalamic-pituitary-adrenocortical and the renin-aldosterone axes. [2] Trilostane effectively blocks the increase in systolic blood pressure and reverses the hypertension produced by drinking 0.9% saline in the Dahlsalt-sensitive rat. Trilostane is equally effective in female and male rats. [3] Trilostane 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] Trilostane results in a reduction in serum cortisol and aldosteroneconcentrations in dogs with PDH, although the decrease for serum aldosterone concentration is smaller than that for serum cortisol concentration. [1]

Protocol (from reference)

References

  • https://pubmed.ncbi.nlm.nih.gov/16806905/
  • https://pubmed.ncbi.nlm.nih.gov/19042143/
  • https://pubmed.ncbi.nlm.nih.gov/15458970/
  • https://pubmed.ncbi.nlm.nih.gov/15478772/
  • https://pubmed.ncbi.nlm.nih.gov/15478772/

Customer Product Validation

Long-time incubations. Spine number in calbindin-labeled PC (red, 7 div) in controls (a), after MLTI (b), MLTI combined with AG205 (c), and MLTI plus trilostane (d); 4d 4 days. Analysis of PC spine number in cell cultures treated with mifepristone in combination with progesterone, AG205, and trilostane at different developmental ages.

Data from [ Cell Mol Life Sci , 2014 , 71(9), 1723-40 ]

In Senegalese sole both recombinant gonadotropins stimulate testosterone and 11-KT production in vitro. The amounts of testosterone and 11-KT were measured in incubation media after 24 h of exposure of testis explants at stage I–II or III to 100 ng/ml of rFsh and rLh, in the presence or absence of 5 uM of inhibitors of the cAMP/PKA pathway (MDL and H-89 respectively) and Hsd-3β (TRIL). Values (mean±S.E.M.) are from three independent experiments on three different males, each with three replicates per condition. Asterisks denote significant differences (P<0.01) with respect to the groups treated with the inhibitors, or as indicated.

Data from [ J Mol Endocrinol , 2014 , 53(2), 175-90 ]

<p>Effects of inhibitors of adenylyl cyclase (MDL-12330A; MDL), PKA (H-89), or 3b -Hsd (TRIL) on gonadotropin-stimulated androgen release by Senegalese sole testicular explants. Amounts of T ( A) and 11-KT (B) measured in incubation media after 24 h of exposure to 250 ng/ml rFsh or rLh, and in combination with 1 or 5 lM MDL-12330A, H-89, or TRIL. Values (mean 6 SEM) represent compiled data from two experiments on two different males, each with three replicates per condition.</p>

Data from [ Biol Reprod , 2012 , 87, 35 ]

Hepatocytes were pre-treated with vehicle or 10 μM Trilostane for 1 h, followed by the addition of 100 μM DHEA for 24 h. Triglyceride content was determined using commercial kits; samples were stained with Oil Red O and photomicrographs were taken to determine the accumulation of lipid droplets, and protein expression of AMPKα, p-AMPKα, ACCα, and p-ACCαwas determined by western blot. E: Immunoblot of AMPKα, p-AMPKα, ACCα, and p-ACCα expression; F: p-AMPK/AMPK protein expression; G: p-ACC/ACC protein expression. Values represent mean ± SE. **P < 0.01 and *P < 0.05, compared to the respective control group.

Data from [ , , Biochim Biophys Acta Mol Cell Biol Lipids, 2018, 1863(6):625-638 ]

Selleck's Trilostane has been cited by 9 publications

Trilostane, a 3β-hydroxysteroid dehydrogenase inhibitor, suppresses growth of hepatocellular carcinoma and enhances anti-cancer effects of sorafenib [ Invest New Drugs, 2021, 10.1007/s10637-021-01132-3] PubMed: 34031786
Dehydroepiandrosterone Prevents H2O2-Induced BRL-3A Cell Oxidative Damage through Activation of PI3K/Akt Pathways rather than MAPK Pathways. [ Oxid Med Cell Longev, 2019, 10.1155/2019/2985956] PubMed: 31182991
Dehydroepiandrosterone reduces accumulation of lipid droplets in primary chicken hepatocytes by biotransformation mediated via the cAMP/PKA-ERK1/2 signaling pathway [Li L Biochim Biophys Acta Mol Cell Biol Lipids, 2018, 1863(6):625-638] PubMed: 29571766
The Adrenal Lipid Droplet is a New Site for Steroid Hormone Metabolism [Yu J Proteomics, 2018, 18(23):e1800136] PubMed: 30358111
Gonadotropin-Activated Androgen-Dependent and Independent Pathways Regulate Aquaporin Expression during Teleost (Sparus aurata) Spermatogenesis [Boj M PLoS One, 2015, 10(11):e0142512] PubMed: 26575371
Gonadotropin-Activated Androgen-Dependent and Independent Pathways Regulate Aquaporin Expression during Teleost (Sparus aurata) Spermatogenesis. [Boj M, et al. PLoS One, 2015, 10(11):e0142512] PubMed: 26575371
Long-term incubation with mifepristone (MLTI) increases the spine density in developing Purkinje cells: new insights into progesterone receptor mechanisms. [Wessel L, et al. Cell Mol Life Sci, 2014, 71(9):1723-40] PubMed: 23982753
Fsh and Lh direct conserved and specific pathways during flatfish semicystic spermatogenesis [Chauvigne F et al. J Mol Endocrinol, 2014, 53(2):175-90] PubMed: 25024405
Follicle-Stimulating Hormone and Luteinizing Hormone Mediate the Androgenic Pathway in Leydig Cells of an Evolutionary Advanced Teleost. [Chauvigné F, et al. Biol Reprod, 2012, 87(2):35] PubMed: 22649073

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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