化合物 (S)-Orteronel|T6051|TargetMol

价格	￥2174
包装	10mg

最小起订量	1mg
发货地	上海
更新日期	2025-06-17

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产品详情

中文名称:化合物 (S)-Orteronel	英文名称:Orteronel
CAS:566939-85-3	品牌: TargetMol
产地: 美国	保存条件: Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
产品类别: 抑制剂
货号: T6051

Product Introduction

Bioactivity

Name	Orteronel
Description	Orteronel ((S)-Orteronel)(TAK-700) was selected as a candidate for clinical evaluation. orteronel (TAK-700) is currently in phase III clinical trials for the treatment of castration-resistant prostate cancer.
Kinase Assay	Rat 11-hydroxylase activity is measured according to a method described for side-chain cleavage activity previously with some modifications. The reaction mixture contained 200 mM mannitol, 4.5 mM HEPES, 2.3 mM potassium phosphate (pH 7.4), 0.1 mM EDTA·2 K, 0.03% BSA (crystallized), 4.5 mM NADPH, 11 mM calcium chloride, 4 μg of mitochondria protein, 10 nM [1,2-3H]-hydroxy-11-deoxycorticosterone (11-deoxycortisol) (NEN, dissolved in 0.02% Tween-80), and 1-1000 nM test compounds in a total volume of 150 μL. The concentrations of reagents are expressed as the final concentration in the reaction mixture. The test compounds are serially diluted with dimethylformamide, and 1.5 μL is added directly to the reaction mixture. After 30 min incubation at 37°C the reaction is terminated by addition of 400 μL of ethyl acetate and 100 μL of distilled water, then vortexed for 30 s and briefly centrifuged. Three hundred μLs of the organic phase is transferred to a new tube and evaporated until dry using nitrogen gas. The steroids are dissolved with 30 μL of ethyl acetate and the whole volume is applied to silica gel TLC plates. The substrate and the products (11-deoxycortisol and cortisol) are separated in the toluene-acetone (7:2) solvent system.
In vitro	In monkey adrenal cells, orteronel inhibits the ACTH stimulated production of DHEA and androstenedione with IC50 of 110 nM and 130 nM, respectively. Furthermore, Orteronel also potently inhibits DHEA production in human adrenocortical tumor line H295R cells with IC50 of 37 nM[1]. In vitro, orteronel shows the potent inhibitory activity against rat and human steroid 17,20-lyase with IC50 of 54 nM and 38 nM, respectively. While other CYP isoforms including 11-hydroxylase and CYP3A4 are not significantly affected by Orteronel. In microsomes expressing human CYP isoforms, Orteronel exhibit greater inhibitory effects on 17,20-lyase with IC50 of 19 nM compared to the other CYP isoforms[2].
In vivo	Orteronel (1 mg/kg, p.o.) results in favorable pharmacokinetic parameters with Tmax, Cmax, t1/2 and AUC0-24 hours of 1.7 hours, 0.147 μg/mL, 3.8 hours and 0.727 μg/mL, respectively[1]. The oral treatment of Orteronel at a dose of 1 mg/kg markedly reduces serum testosterone and dehydroepiandrosterone (DHEA) levels in cynomolgus monkeys[2].
Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
Solubility Information	H2O : <1 mg/mL Ethanol : 8 mg/mL (26.02 mM) DMSO : 61 mg/mL (198.47 mM)
Keywords	CYPs \| Inhibitor \| TAK 700 \| Cytochrome P450 \| inhibit \| Orteronel \| TAK700
Inhibitors Related	Naringin \| 1-Aminobenzotriazole \| Gemfibrozil \| Fenofibrate \| Tauroursodeoxycholate \| Methoxsalen \| Doxepin hydrochloride \| Naringenin \| Apigenin \| 1-Ethynylnaphthalene \| Tebuconazole \| Diflubenzuron

关键字： TAK-700|||(S)-Orteronel|TargetMol

公司简介

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

成立日期	2013-04-18 （13年）	注册资本	566.265100万人民币
员工人数	100-500人	年营业额	￥ 1亿以上
主营行业	天然产物,生化试剂,分子生物学,分子砌块,生物技术服务	经营模式	贸易,工厂,试剂,定制,服务

TargetMol中国（陶术生物）

VIP 4年

公司成立：13年
注册资本：566.265100万人民币
企业类型：有限责任公司(自然人投资或控股)
主营产品：小分子抑制剂、药物筛选化合物库、药物筛选等
公司地址：静安区江场三路238号8楼

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化合物 (S)-Orteronel|T6051|TargetMol相关厂家报价

产品名称	价格		公司名称	报价日期
人17，20-裂解酶(17,20-lyase)抑制剂(Orteronel)	询价	VIP6年	上海泽叶生物科技有限公司	2025-06-20
TAK-700 (Orteronel)	询价		南京百鑫德诺生物科技有限公司	2024-09-26
TAK-700 (S-form	询价		ChemScene, LLC	2016-06-18
TAK-700	询价		上海蓝木化工有限公司	2012-05-29
TAK-700	询价		Biotool LLC	2012-05-28
TAK-700	询价		Selleckchem LLC	2012-05-28

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