化合物 (S)-Orteronel|T6051|TargetMol

價(jià)格	￥2174
包裝	10mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2025-07-16

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產(chǎn)品詳情

中文名稱(chēng):化合物 (S)-Orteronel	英文名稱(chēng):Orteronel
CAS:566939-85-3	品牌: TargetMol
產(chǎn)地: 美國(guó)	保存條件: Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
產(chǎn)品類(lèi)別: 抑制劑
貨號(hào): T6051

Product Introduction

Bioactivity

名稱(chēng)	Orteronel
描述	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.
激酶實(shí)驗(yàn)	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.
體外活性	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].
體內(nèi)活性	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].
存儲(chǔ)條件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
溶解度	H2O : <1 mg/mL Ethanol : 8 mg/mL (26.03 mM), Sonication is recommended. DMSO : 61 mg/mL (198.47 mM), Sonication is recommended.
關(guān)鍵字	TAK700 \| TAK 700 \| Orteronel \| Inhibitor \| inhibit \| human 17 (20-lyase) \| Cytochrome P450 \| CYPs
相關(guān)產(chǎn)品	Naringin \| 1-Aminobenzotriazole \| Gemfibrozil \| Fenofibrate \| Tauroursodeoxycholate \| Benzbromarone \| Methoxsalen \| Naringenin \| Apigenin \| 1-Ethynylnaphthalene \| Tebuconazole \| Diflubenzuron

關(guān)鍵字： TAK-700|||(S)-Orteronel|TargetMol

公司簡(jiǎn)介

TargetMol Chemicals Inc. 總部位于馬薩諸塞州波士頓，致力于為全球生化領(lǐng)域科學(xué)家的研究提供專(zhuān)業(yè)的產(chǎn)品和服務(wù)。TargetMol?品牌的客戶(hù)群分布于40多個(gè)國(guó)家和地區(qū)，已發(fā)展成為全球知名的化合物庫(kù)和小分子化合物研究供應(yīng)商。 TargetMol?可提供160多種滿(mǎn)足不同需求的化合物庫(kù)，以及多種類(lèi)型的生化試劑產(chǎn)品，包括12000多種抑制劑、16000多種天然產(chǎn)物和各類(lèi)多肽、抗體、生命科學(xué)試劑盒等，此外，我們還建設(shè)有CADD（計(jì)算機(jī)輔助藥物設(shè)計(jì)）研究中心、藥理實(shí)驗(yàn)室、藥化合成平臺(tái)三大技術(shù)中心，全方位滿(mǎn)足客戶(hù)的定制需求。憑借我們優(yōu)質(zhì)的產(chǎn)品和服務(wù)、快速高效的全球供應(yīng)鏈和專(zhuān)業(yè)的技術(shù)支持，我們將有效幫助您縮短研發(fā)周期，取得更成功的結(jié)果。

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公司成立：13年
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