Trilostane

Catalog No.S1404 Synonyms: WIN 24540

Trilostane Chemical Structure

Molecular Weight(MW): 329.43

Trilostane is an inhibitor of 3β-hydroxysteroid dehydrogenase used in the treatment of Cushing’s syndrome.

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4 Customer Reviews

  • 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.

    Cell Mol Life Sci 2014 71(9), 1723-40. Trilostane purchased from Selleck.

    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.

    Biol Reprod 2012 87, 35 . Trilostane purchased from Selleck.

  • 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.

    J Mol Endocrinol 2014 53(2), 175-90. Trilostane purchased from Selleck.

    Effect of the steroidogenesis inhibitor TRIL on gonadotropin-induced androgen production and aquaporin transcriptional regulation in vitro. (A, C-D, J) Amounts of T (A, C, J) and 11-KT (D) released into the incubation media by explants at the resting, spermatogenic and spermiation stages after 24 h exposure to 100 ng/ml rFsh or rLh, or hormone vehicle (control; C), in the presence or absence of 5 μM TRIL. (B, E-H, K-L) Effect of TRIL on rFsh and rLh-induced aquaporin gene expression during spermatogenesis. Data are represented as in Fig 3. Dashed line at mRNA level 1 indicates no change with respect time zero. Values (mean ± S.E.M.) represent compiled data from two experiments on two different pools of males or individual males, each with three replicates per treatment. *, P < 0.05; **, P < 0.01, with respect the control group not treated with TRIL, or as indicated in brackets.

    PLoS One, 2015, 10(11):e0142512.. Trilostane purchased from Selleck.

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Biological Activity

Description Trilostane 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

Solubility (25°C)

In vitro DMSO 65 mg/mL (197.31 mM)
Water Insoluble
Ethanol 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.

Chemical Information

Molecular Weight 329.43
Formula

C20H27NO3

CAS No. 13647-35-3
Storage powder
Synonyms WIN 24540

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01615211 Terminated Medical Abortion, Complete or Unspecified, Without Complication Kristina Gemzell Danielsson|Karolinska Institutet|The University of Hong Kong May 2012 Phase 2
NCT00181597 Completed Prostate Cancer|Prostate Adenocarcinoma Genzyme, a Sanofi Company|Sanofi March 2004 Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Dehydrogenase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID