化合物 Tiplaxtinin|T2030|TargetMol

價(jià)格	￥235	￥333	￥543
包裝	1mg	2mg	5mg

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:化合物 Tiplaxtinin	英文名稱:Tiplaxtinin
CAS:393105-53-8	品牌: TargetMol
產(chǎn)地: 美國	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: 99.49%	產(chǎn)品類別: 抑制劑
貨號(hào): T2030

Product Introduction

Bioactivity

名稱	Tiplaxtinin
描述	Tiplaxtinin (Tiplasinin)(PAI-039) is a selective and orally efficacious inhibitor of plasminogen activator inhibitor-1 (PAI-1) with IC50 of 2.7 uM.
細(xì)胞實(shí)驗(yàn)	Briefly, cell lines, T24, UM-UC-14, UROtsa, and HeLa cells are plated in 96-well dishes in triplicate at 1×103 cells per well and allowed to adhere for 24 hours. Subsequently, tiplaxtinin is added to the wells and allowed to incubate at the indicated concentrations. Cellular proliferation is determined by CellTiter-Glo Luminescent Cell Viability Assay according to manufacturer's instructions at 24 hours, and IC50 of tiplaxtinin is determined in Graphpad Prism. Luminescence was measured using a FLUOstar OPTIMA Reader.(Only for Reference)
激酶實(shí)驗(yàn)	Direct PAI-I in vitro activity assays : The chromogenic assay is initiated by the addition of tiplaxtinin (10 – 100 μM final concentration, maximum DMSO concentration of 0.2%) to recombinant human PAI-1 (140 nM in pH 6.6 buffer). After a 15 minute incubation at 25°C, 70 nM of recombinant human t-PA is added, and the combination of tiplaxtinin, PAI-1 and tPA are incubated for an additional 30 minutes. After the second incubation, Spectrozyme tPA, is added and absorbance read at 405 nm at 0 and 60 minutes. Relative PAI-1 inhibitory activity is equal to the residual tPA activity in the tiplaxtinin / PAI-1 treatment. Control treatments include the complete inhibition of tPA by PAI-1 at the molar ratio employed (2:1), and the absence of any effect of the tiplaxtinin on t-PA alone. The immunofunctional assay is based upon the non-SDS dissociable interaction between tPA and active PAI-1. Assay plates are coated with 100 μl of a solution of t-PA (10 μg/ml in TBS), and kept at 4 °C overnight. Tiplaxtinin is dissolved in DMSO and diluted to a final concentration of 1-100 μM as described above. Tiplaxtinin is then incubated with human PAI-1 (50 ng/ml) for 15 minutes, and an aliquot of this solution added to the t-PA-coated plate for 1 h. The solution is aspirated from the plate, which is then washed with a buffer consisting of 0.05% Tween 20 and 0.1% BSA in TBS. This assay detects only active inhibitory PAI-1 (not latent or substrate) bound to the plate, and is quantitated using a monoclonal antibody against human PAI-1 (MA33B8). A 1000X dilution of MA33B8 is added to the plate and incubated at for one hour, aspirated and washed. A secondary antibody consisting of goat anti-mouse IgG (H+L)-AP alkaline phosphatase conjugate is added, incubated for one hour, aspirated and washed. A 100 μl aliquot of alkaline phosphatase solution is added, followed by determination of absorbance at 405 nm 60 minutes later.The quantitation of residual active PAI-1 bound to t-PA at varying concentrations of tiplaxtinin is used to determine the IC50 by fitting the results to a logistic dose-response program, with the IC50 defined as the concentration of compound required to achieve 50% inhibition of PAI-1 activity. The assay sensitivity is 5 ng/ml of human PAI-1 as determined from a standard curve ranging from 0-100 ng/ml of human PAI-1.
體外活性	在一系列人類膀胱細(xì)胞系中，PAI-1導(dǎo)致細(xì)胞增殖、細(xì)胞黏附和群體形成的減少，并引發(fā)凋亡和脫落性凋亡。[4]
體內(nèi)活性	在大鼠頸動(dòng)脈血栓模型中，Tiplaxtinin（1 mg/kg，口服）延長(zhǎng)了血栓閉塞時(shí)間，并阻止了頸動(dòng)脈血流量減少。[1] 在C57BL/6J小鼠中，Tiplaxtinin（1 mg/g飼料）減輕了Ang II引起的主動(dòng)脈重塑。[2] 在未經(jīng)治療的1型糖尿病小鼠中，Tiplaxtinin（口服）恢復(fù)了骨骼肌再生。[3] 在攜帶人類癌細(xì)胞系T24和HeLa異種移植物的無胸腺小鼠中，Tiplaxtinin（1 mg/kg，口服）減緩了腫瘤異種移植物的生長(zhǎng)，這與腫瘤血管生成減少、細(xì)胞增殖減少及凋亡增加有關(guān)。[4]
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	H2O : < 1 mg/mL (insoluble or slightly soluble) Ethanol : 15 mg/mL (34.1 mM) DMSO : 50 mg/mL (113.8 mM)
關(guān)鍵字	Inhibitor \| PAI 039 \| Plasminogen activator inhibitor-1 \| inhibit \| PAI-1 \| PAI039 \| Apoptosis \| Tiplaxtinin
相關(guān)產(chǎn)品	Lidocaine hydrochloride \| Metronidazole \| 5-Fluorouracil \| Stavudine \| Tributyrin \| Dextran sulfate sodium salt (MW 4500-5500) \| Myricetin \| Sorafenib \| L-Ascorbic acid \| Acetylcysteine \| Sodium 4-phenylbutyrate \| Kaempferol
相關(guān)庫	抑制劑庫 \| 經(jīng)典已知活性庫 \| 已知活性化合物庫 \| 代謝化合物庫 \| 含氟化合物庫 \| 細(xì)胞凋亡化合物庫 \| NO PAINS 化合物庫 \| 臨床期小分子藥物庫 \| 口服活性化合物庫 \| 藥物功能重定位化合物庫

關(guān)鍵字： PAI-039|||Tiplasinin|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)家的研究提供專業(yè)的產(chǎn)品和服務(wù)。TargetMol?品牌的客戶群分布于40多個(gè)國家和地區(qū)，已發(fā)展成為全球知名的化合物庫和小分子化合物研究供應(yīng)商。 TargetMol?可提供160多種滿足不同需求的化合物庫，以及多種類型的生化試劑產(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，全方位滿足客戶的定制需求。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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