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Trilostane
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Trilostane图片
CAS NO:13647-35-3
规格:≥98%
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议
1g电议
2g电议
5g电议

产品介绍
理化性质和储存条件
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)[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

SynonymsWIN 24540; WIN24540; Trilostane; D 01180; Modrastane. Desopan; DB011080; WIN-24540; D-01180; Modrenal.
实验参考方法
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.