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曲洛司坦 /Trilostane {[allProObj[0].p_purity_real_show]}

货号:A378777 同义名: 曲洛斯坦 / Win 24540;Desopan

Trilostane is an inhibitor of 3 β-hydroxysteroid dehydrogenase for Cushing's syndrome.

Trilostane 化学结构 CAS号:13647-35-3
Trilostane 化学结构
CAS号:13647-35-3
Trilostane 3D分子结构
CAS号:13647-35-3
Trilostane 化学结构 CAS号:13647-35-3
Trilostane 3D分子结构 CAS号:13647-35-3
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Trilostane 纯度/质量文件 产品仅供科研

货号:A378777 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Dehydrogenase 其他靶点 纯度
Trilostane 99+%
AGI-6780 +++

IDH2 R140Q mutant, IC50: 23 nM

99%+
Gimeracil 98%
AGI-5198 ++

R132H-IDH1, IC50: 70 nM

R132C-IDH1, IC50: 0.16 μM

99%+
SW033291 ++++

15-PGDH, IC50: 1.5 nM

15-PGDH, Ki: 0.1 nM

99%+
Mycophenolic acid 99+%
Fomepizole 98%
Leflunomide 98%
3-Nitropropanoic acid 99%+
Isovaleramide 98%
Mycophenolate Mofetil +++

Inosine monophosphate dehydrogenase I, IC50: 39 nM

Inosine monophosphate dehydrogenase II, IC50: 27 nM

98%
MK-8245 ++++

SCD1 (rat), IC50: 3 nM

SCD1 (mouse), IC50: 1 nM

99%+
Vidofludimus ++

Human DHODH, IC50: 134 nM

99%+
Emodin 98%
Ivosidenib 98%
NCT-501 ++

ALDH1A1, IC50: 40 nM

98%
Gossypol 99%+
Devimistat 98%
Disulfiram 98%+
Enasidenib ++++

IDH2, IC50: 12 nM

98%
PluriSIn 1 99%+
ML390 +

DHODH, IC50: 0.56 μM

99%+
Teriflunomide 99%+
Daidzin +++

ALDH-Ⅰ, Ki: 20 nM

98+%
18β-Glycyrrhetinic acid 99%
RRx-001 95%
NCT-503 +

PHGDH, IC50: 2.5 μM

99%+
Vorasidenib 99%+
Ammonium Glycyrrhizinate(x:1) 98+%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Trilostane 生物活性

靶点
  • Dehydrogenase

描述 Trilostane is a recognized treatment for canine pituitary-dependent hyperadrenocorticism (PDH); The median survival time for animals treated with trilostane was 353 days (95% confidence interval [CI] 95-528 days)[3]. During trilostane therapy, urinary catecholamines and their metabolites did not decrease significantly. However, dogs with low post-ACTH cortisol concentrations during trilostane therapy had less increased epinephrine, norepinephrine and normetanephrine, creatinine ratios compared to healthy dogs[4]. In a substantial number of dogs treated with trilostane, the two prepill cortisol concentrations differed. Part of this difference might be ascribable to stressful events during test performance[5].

Trilostane 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01615211 Medical Abortion, Complete or ... 展开 >>Unspecified, Without Complication 收起 << Phase 2 Terminated(No access to study ... 展开 >>drug Trilostan. Company closed down) 收起 << - Sweden ... 展开 >> Karolinska University Hospital Stockholm, Sweden, 17177 收起 <<
NCT00181597 Prostate Cancer ... 展开 >> Prostate Adenocarcinoma 收起 << Phase 2 Completed - United States, Massachusetts ... 展开 >> Massachusetts General Hospital Boston, Massachusetts, United States, 02114 Dana-Farber Cancer Institute Boston, Massachusetts, United States, 02115 收起 <<

Trilostane 参考文献

[1]Feldman EC, Kass PH. Trilostane dose versus body weight in the treatment of naturally occurring pituitary-dependent hyperadrenocorticism in dogs. J Vet Intern Med. 2012 Jul-Aug;26(4):1078-80.

[2]Helm JR, McLauchlan G, et al. A comparison of factors that influence survival in dogs with adrenal-dependent hyperadrenocorticism treated with mitotane or trilostane. J Vet Intern Med. 2011 Mar-Apr;25(2):251-60.

[3]Helm JR, McLauchlan G, Boden LA, Frowde PE, Collings AJ, Tebb AJ, Elwood CM, Herrtage ME, Parkin TD, Ramsey IK. A comparison of factors that influence survival in dogs with adrenal-dependent hyperadrenocorticism treated with mitotane or trilostane. J Vet Intern Med. 2011 Mar-Apr;25(2):251-60

[4]Sieber-Ruckstuhl N, Salesov E, Quante S, Riond B, Rentsch K, Hofmann-Lehmann R, Reusch C, Boretti F. Effects of Trilostane on urinary Catecholamines and their metabolites in dogs with Hypercortisolism. BMC Vet Res. 2017 Sep 4;13(1):279

[5]Boretti F, Musella C, Burkhardt W, Kuemmerle-Fraune C, Riond B, Reusch C, Sieber-Ruckstuhl N. Comparison of two prepill cortisol concentrations in dogs with hypercortisolism treated with trilostane. BMC Vet Res. 2018 Dec 27;14(1):417

Trilostane 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.04mL

0.61mL

0.30mL

15.18mL

3.04mL

1.52mL

30.36mL

6.07mL

3.04mL

Trilostane 技术信息

CAS号13647-35-3
分子式C20H27NO3
分子量 329.433
别名 曲洛斯坦 ;Win 24540;Desopan;Modrenal.;Modrastane. Desopan;D-01180;DB01108;Vetoryl;Modrefen
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C

溶解度

DMSO: 55 mg/mL(166.95 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方

IP 2% DMSO+2% Tween80+40% PEG300+water 2 mg/mL clear

PO 0.5% CMC-Na 42 mg/mL suspension

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