化合物 TP0463518|T5392|TargetMol

價(jià)格	￥593	￥1490	￥2320
包裝	1mg	5mg	10mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-09-29

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產(chǎn)品詳情

中文名稱(chēng):化合物 TP0463518	英文名稱(chēng):TP0463518
CAS:1558021-37-6	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.
純度規(guī)格: 99.43%	產(chǎn)品類(lèi)別: 抑制劑
貨號(hào): T5392

Product Introduction

Bioactivity

名稱(chēng)	TP0463518
描述	TP-0463518 is a highly potent HIF prolyl hydroxylase (PHD) inhibitor (IC50s: 13 nM and 18 nM for human and rat PHD2, respectively).
激酶實(shí)驗(yàn)	The PHDs inhibition studies were performed using fluorescence polarization.FITC-HIF and 2-oxoglutarate were mixed with enzyme solution in a reaction buffer (20 mM Tris-HCl [pH 7.5],5 mM KCl,1.5 mM MgCl2,10 μM FeSO4,2 mM ascorbic acid,1 mM DTT) with or without various concentrations of TP0463518.The concentrations of FITC-HIF and 2-oxoglutarate were twice the Km values of each enzyme.The reaction temperature was 30?C,and the reaction time was optimized to each PHD enzyme to obtain the initial velocity (9 to 20 min).At the end of the reaction,a stop solution containing 20 mM of EDTA and anti-hydroxylated HIF antibody was added to the reaction buffer.Then,the fluorescence (ex: 480 nm,em: 535 nm) was measured using EnVision to calculate the millipolarization (mP) value.The mP values and the corresponding hydroxylated HIF concentration were proportional,so we used the mP values as the activities.The IC50 values were calculated using SAS version 9.2 using a nonlinear least-squares method.To determine the mode of inhibition,the activity of PHD2 was measured with various concentrations of 2-oxoglutarate (0.025 to 8 μM) and TP0463518 (0 to 40 μM).Then the apparent Vmax and Km corresponding to each TP0463518 concentration were compared.The mode of inhibition was confirmed using a double reciprocal plot.
動(dòng)物實(shí)驗(yàn)	Nine-week-old Balb/c mice were randomly assigned to a vehicle or a 5 to 40 mg/kg dose of TP0463518 group. The mice were orally treated with 0.5% methylcellulose or a TP0463518 dosing suspension. Blood was collected at 6 h after administration from the orbital plexus under deep anesthesia, and euthanasia was performed without awakening. An aliquot of blood was mixed with EDTA, and the remaining blood sample was left to stand at room temperature for 15 min. The samples were then centrifuged (2130 x g for 10 min at 4°C) to prepare the plasma and serum.
體外活性	TP0463518 競(jìng)爭(zhēng)性抑制人類(lèi) PHD2，Ki 值為 5.3nM。此外，TP0463518 也對(duì)人類(lèi) PHD1/3 表現(xiàn)出抑制作用，IC50 值分別為 18 nM 和 63 nM，以及對(duì)猴子 PHD2 的抑制作用，IC50 值為 22nM。
體內(nèi)活性	在正常的小鼠和大鼠中，TP0463518在5mg/kg和20mg/kg的劑量下顯著提高了血清EPO水平。在5/6腎切除的慢性腎臟病模型大鼠中，TP0463518以10mg/kg的劑量也增加了血清EPO水平，血清EPO與血清TP0463518水平的相關(guān)系數(shù)為0.82。TP0463518的半衰期為5.2小時(shí)，且在5mg/kg的劑量下增加了EPO的曲線(xiàn)下面積(AUC)。
存儲(chǔ)條件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 110 mg/mL (254.73 mM)
關(guān)鍵字	TP0463518 \| HIF-PH \| TP-0463518 \| HIFs \| TP 0463518 \| inhibit \| Inhibitor \| HIF/HIF Prolyl-Hydroxylase \| Hypoxia-inducible factors
相關(guān)產(chǎn)品	Hydralazine hydrochloride \| Hydroxycitric acid tripotassium hydrate \| Chlorogenic Acid \| Glucosamine \| 1,4-DPCA \| DMOG \| Glucosamine sulfate \| Deferoxamine Mesylate \| Glucosamine hydrochloride \| Vadadustat \| Minocycline hydrochloride \| Oltipraz
相關(guān)庫(kù)	抑制劑庫(kù) \| 經(jīng)典已知活性庫(kù) \| 已知活性化合物庫(kù) \| 抗癌細(xì)胞代謝庫(kù) \| 代謝化合物庫(kù) \| 抗衰老化合物庫(kù) \| HIF-1化合物庫(kù) \| 谷氨酰胺代謝化合物庫(kù) \| NO PAINS 化合物庫(kù) \| 糖代謝化合物庫(kù)

關(guān)鍵字： TP0463518|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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