化合物 TR14035|T5310|TargetMol

價格	￥407	￥942	￥1430
包裝	1mg	5mg	10mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-12-12

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產(chǎn)品詳情

中文名稱:化合物 TR14035	英文名稱:TR-14035
CAS:232271-19-1	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: 99.81%	產(chǎn)品類別: 抑制劑
貨號: T5310

Product Introduction

Bioactivity

名稱	TR-14035
描述	TR-14035 (MDK-1191) is a dual antagonist of α4β7/α4β1 integrins (IC50s: 7/87nM).
細(xì)胞實驗	RPMI8866 cell line and Jurkat T lymphoblastoid cell line were grown as a suspension culture in RPMI 1640 media, 10% FCS, 2 mM glutamine, 100 units/mL penicillin G, 100 mg/mL streptomycin sulfate at 37 °C and 5% CO2. Adhesion assays have been detailed elsewhere. Microtiter plates were coated with 20 mg/mL HSA for 2 h at room temperature, washed once with PBS and derivatized with 10 mg/mL SPDP for 1 h. After washing, CS-1 (or sCS-1) derived peptide solution (100 mL at 100 μg/mL) was added to the wells and allowed to crosslink to the plates overnight at 4 °C. Non-reacted sites were blocked with 100 mL of 1% OV in PBS for 1 h at 37 °C. RPMI8866 cells were suspended in Dulbecco's modified Eagle's medium with 0.25% OV at a density of 2.5 ×106/mL and incubated for ~1 h at 37 °C with varying concentrations of antagonists on peptide-coated plates. Following washing (EL404 plate washer), bound cells were quantified by measuring endogenous N-acetyl-hexosaminidase activity by reading the optical density at 405 nm using the enzyme substrate p-nitrophenol-N-acetyl-b-d-glucoseaminide. IC50 values were generated by nonlinear regression from titration curves of antagonists from seven doses and reported as the average of a minimum of two experiments. Since experimental variability was noted with respect to the IC50 of the internal standard [(1S - cis) - N - [(3 - carboxy - 2,2,3 - trimethylcyclopentyl)- carbonyl]-O-[(2,6-dichlorophenyl)methyl]-l-tyrosine] a normalization procedure was done using the global mean value [IC50=0.224±0.17 μM (N=19)] of the internal standard. For the Jurkat cell adhesion assay, OV was replaced with 0.25% HSA for both blocking and adhesion buffers. Standard error of the mean for the Jurkat cell adhesion assay was typically <10% for each experiment and no normalization was needed [1].
動物實驗	For biliary excretion studies in mice and rats, a cannula (polyethylene tube, SP8 for mice and SP10 for rats) was inserted into the bile duct of the anesthetized animal. In the rat, after complete recovery from diethyl ether anesthesia, TR-14035 was administered intravenously at a dose of 3 mg/ml/kg, and the bile, urine, and blood were collected at designated time intervals. In the mouse, TR-14035 was administered intravenously at a dose of 3 mg/4 ml/kg, and the bile and blood were collected at designated time intervals under pentobarbital anesthesia. Blood was centrifuged to separate plasma, and all the samples were stored at j20 -C until analysis by LC-MSD [2].
體外活性	TR-14035（IC50：alpha(4)beta(7)/alpha(4)beta(1)=7/87 nM）已完成歐洲的第一階段研究[1]。在大鼠和人類肝細(xì)胞中，TR-14035的攝取是通過一個明顯的單一飽和機(jī)制進(jìn)行的，其K(m)分別為6.7和2.1 microM，而?；悄懰岷偷馗咝量梢詼p少這種攝取。在卵母細(xì)胞中表達(dá)的OATP1B1/OATP-C 和 OATP1B3/OATP8介導(dǎo)了TR-14035的攝取，其K(m)分別為7.5和5.3 microM[2]。TR14035阻斷了人類alpha(4)beta(7)與(125)I-MAdCAM-Ig融合蛋白的結(jié)合，IC(50)值為0.75 nM。在體外剪切流條件下，TR14035阻斷了表達(dá)人類alpha(4)beta(7)的RPMI-8866細(xì)胞或小鼠腸系膜淋巴結(jié)淋巴細(xì)胞與MAdCAM-Ig的結(jié)合，IC(50)值為0.1 microM[3]。
體內(nèi)活性	在EHBRs中，未變化的TR-14035的膽汁排泄和全身清除率顯著低于正常大鼠，而在野生型與mdr1a/b-或Bcrp基因敲除小鼠之間，清除率無顯著差異[2]。TR14035阻斷了對HEVs的粘附(ED50：0.01-0.1 mpk i.v.)[3]。
存儲條件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	H2O : Insoluble DMSO : 40 mg/Ml (84.3 mM)
關(guān)鍵字	MDK1191 \| autoimmune \| TR-14035 \| disease \| asthma \| Integrin \| inhibit \| MDK 1191 \| TR 14035 \| allergic \| TR14035 \| inflammation \| Inhibitor \| alpha(4)
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關(guān)鍵字： MDK-1191|TargetMol

公司簡介

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（計算機(jī)輔助藥物設(shè)計）研究中心、藥理實驗室、藥化合成平臺三大技術(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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公司成立：12年
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主營產(chǎn)品：小分子抑制劑、藥物篩選化合物庫、藥物篩選等
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