化合物 TP0463518|T5392|TargetMol

TP0463518
1558021-37-6

￥593 1mg 起订

￥1490 5mg 起订

￥2320 10mg 起订

上海更新日期：2024-12-12

TargetMol中国（陶术生物）

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联系人：邵小姐

手机：4008200310 拨打

邮箱：marketing@tsbiochem.com

产品详情:

中文名称：: 化合物 TP0463518

英文名称：: TP0463518

CAS号：: 1558021-37-6

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.

纯度规格：: 99.43%

产品类别：: 抑制剂

货号：: T5392

Product Introduction

Bioactivity

名称	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).
激酶实验	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.
动物实验	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.
体外活性	TP0463518 竞争性抑制人类 PHD2，Ki 值为 5.3nM。此外，TP0463518 也对人类 PHD1/3 表现出抑制作用，IC50 值分别为 18 nM 和 63 nM，以及对猴子 PHD2 的抑制作用，IC50 值为 22nM。
体内活性	在正常的小鼠和大鼠中，TP0463518在5mg/kg和20mg/kg的剂量下显著提高了血清EPO水平。在5/6肾切除的慢性肾脏病模型大鼠中，TP0463518以10mg/kg的剂量也增加了血清EPO水平，血清EPO与血清TP0463518水平的相关系数为0.82。TP0463518的半衰期为5.2小时，且在5mg/kg的剂量下增加了EPO的曲线下面积(AUC)。
存储条件	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)
关键字	TP0463518 \| HIF-PH \| TP-0463518 \| HIFs \| TP 0463518 \| inhibit \| Inhibitor \| HIF/HIF Prolyl-Hydroxylase \| Hypoxia-inducible factors
相关产品	PX-478 \| Hydralazine hydrochloride \| Hydroxycitric acid tripotassium hydrate \| Chlorogenic Acid \| Glucosamine \| Chloramphenicol \| 1,4-DPCA \| Glucosamine sulfate \| Deferoxamine Mesylate \| Glucosamine hydrochloride \| Minocycline hydrochloride \| Oltipraz
相关库	抑制剂库 \| 经典已知活性库 \| 已知活性化合物库 \| 抗癌细胞代谢库 \| 代谢化合物库 \| 抗衰老化合物库 \| HIF-1化合物库 \| 谷氨酰胺代谢化合物库 \| NO PAINS 化合物库 \| 糖代谢化合物库

TP0463518|TargetMol

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。

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