product name Trilostane
Description: Trilostane (also known as WIN 24540) is a potent inhibitor of 3β-hydroxysteroid dehydrogenase that is used in the treatment of Cushing’s syndrome. It was withdrawn from the human market of US in April 1994 but was recently approved in 2008 as a veterinary drug for the treatment of Cushings disease (hyperandrenocorticism) in dogs. It is also the first drug approved to treat both pituitary- and adrenal-dependent Cushings in dogs.
References: J Steroid Biochem Mol Biol. 2006 Aug;100(4-5):141-51; Vet J. 2010 Jan;183(1):75-80.
329.43
Formula
C20H27NO3
CAS No.
13647-35-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 65 mg/mL (197.3 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
WIN 24540
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19410151
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. 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. 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. 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. |
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| Formulation & Dosage | |
| References | J Steroid Biochem Mol Biol. 2006 Aug;100(4-5):141-51; Vet J. 2010 Jan;183(1):75-80; Am J Physiol Regul Integr Comp Physiol. 2005 Feb;288(2):R389-93. |
