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Merck
CN

SML0141

Sigma-Aldrich

Trilostane

≥98% (HPLC), 3β-hydroxysteroid dehydrogenase inhibitor, powder

别名:

(4α,5α,17β)-3,17-dihydroxy-4,5-epoxyandrost-2-ene-2-carbonitrile

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关于此项目

经验公式(希尔记法):
C20H27NO3
化学文摘社编号:
分子量:
329.43
EC 号:
MDL编号:
UNSPSC代码:
51111800
PubChem化学物质编号:
NACRES:
NA.77
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产品名称

Trilostane, ≥98% (HPLC)

方案

≥98% (HPLC)

表单

powder

颜色

white to tan

溶解性

DMSO: ≥17 mg/mL

储存温度

2-8°C

SMILES字符串

C[C@]12CC[C@H]3[C@@H](CC[C@@]45O[C@@H]4C(O)=C(C[C@]35C)C#N)[C@@H]1CC[C@@H]2O

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

InChI key

KVJXBPDAXMEYOA-CXANFOAXSA-N

基因信息

human ... HSD3B2(3284)

一般描述

Trilostane inhibits the production of adrenal steroids, such as cortisol and aldosterone. It is used to treat aldosteronism.

应用

Trilostane has been used to evaluate its capability to regulate the sex-dependent differences in the lipopolysaccharide (LPS)-induced inflammatory responses of astrocytes.
Trilostane was used to inhibit the activity of 3β-hydroxysteroid dehydrogenase in mouse ovary.

生化/生理作用

Inhibitor of 3 β-hydroxysteroid dehydrogenase
Trilostane is an inhibitor of 3 β-hydroxysteroid dehydrogenase (3-β-HSD or delta 5-delta 4-isomerase), an essential enzyme for the biosynthesis of all classes of hormonal steroids. It has been used in the treatment of Cushing′s syndrome for stopping the production of cortisol, and is currently approved for dogs in the US, but is still a human drug in the UK and other countries. It is being investigated as a possible treatment for both breast cancer and prostate cancer to prevent the synthesis of estrogens and androgens from endogenous precursors. It has also been used to inhibit endogenous production of progesterone in research studies.

特点和优势

This compound is featured on the Nuclear Receptors (Steroids) page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

象形图

Health hazardExclamation mark

警示用语:

Warning

危险声明

危险分类

Eye Irrit. 2 - Repr. 2 - Skin Irrit. 2

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

法规信息

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历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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Edward C Feldman
Journal of the American Veterinary Medical Association, 238(11), 1441-1451 (2011-06-02)
To evaluate effectiveness and incidence of adverse reactions to twice-daily lower-dose oral administration of trilostane in the treatment of dogs with naturally occurring hyperadrenocorticism (NOH). Clinical trial. 47 dogs with NOH. 47 dogs were treated orally with trilostane (0.21 to
K-D Cho et al.
Journal of veterinary internal medicine, 27(1), 91-98 (2012-11-22)
Trilostane is commonly used to treat pituitary-dependent hyperadrenocorticism (PDH) in dogs. There are differing opinions regarding the dose and frequency of trilostane administration in dogs with PDH. To compare the efficacy of 2 trilostane protocols in the treatment of dogs
Nyssa J Reine
Clinical techniques in small animal practice, 22(1), 18-25 (2007-06-05)
Pituitary-dependent hyperadrenocorticism is a common endocrine disorder in dogs in the United States. Once a diagnosis is established, a decision must be made whether or not to pursue treatment, and if so, which medication to use. Historically, mitotane (Lysodren, o,p'-DDD
Julie Espallergues et al.
Neuropharmacology, 62(1), 492-502 (2011-09-29)
In the present study, we analyzed the effects of a systemic treatment with the competitive 3β-hydroxysteroid dehydrogenase (3β-HSD) inhibitor trilostane on: (i) neurosteroid and monoamine levels in the brain, and (ii) the antidepressant activity of steroids and antidepressants in the
Yu Chien et al.
Biology of reproduction, 89(4), 91-91 (2013-08-24)
Normal pregnancy is supported by increased levels of progesterone (P4), which is secreted from ovarian luteal cells via enzymatic steps catalyzed by P450scc (CYP11A1) and HSD3B. The development and maintenance of corpora lutea during pregnancy, however, are less well understood.

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