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    Trilostane
    Trilostane

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0860
    CAS #: 13647-35-3Purity ≥98%

    Description: 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 However, Trilostane was withdrawn from the United States in the 1990s and was later approved as a veterinary medicine for use in the treatment of Cushing's syndrome in dogs. 

    References: J Steroid Biochem Mol Biol. 2006 Aug;100(4-5):141-51; Vet J. 2010 Jan;183(1):75-80.  

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    Molecular Weight (MW)329.43
    FormulaC20H27NO3
    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)

    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)[[email protected]@]2([H])O[[email protected]@]23[[email protected]]([[email protected]@]4([H])CC[[email protected]@]5(C)[[email protected]](CC[[email protected]@H]5O)([H])[[email protected]]4([H])CC3)(C)C1           

    SynonymsWIN 24540; WIN24540; Trilostane; D 01180; Modrastane. Desopan; DB011080; WIN-24540; D-01180; Modrenal.


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    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.

    In VivoTrilostane 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.
    Animal modelDogs
    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.


    These protocols are for reference only. InvivoChem does not independently validate these methods.


    Systolic blood pressure measured by tail cuff in female SS/jrctr rats drinking 0.9% NaCl and eating standard chow ad libitum. Am J Physiol Regul Integr Comp Physiol. 2005 Feb;288(2):R389-93.
     
    Systolic blood pressure measured by tail cuff in male SS/jrctr rats drinking 0.9% NaCl and eating standard chow ad libitum. Am J Physiol Regul Integr Comp Physiol. 2005 Feb;288(2):R389-93.


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