化合物 MK-7246|TQ0051|TargetMol

價(jià)格	￥6910	￥1550	￥12200
包裝	5mg	1mg	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 MK-7246	英文名稱:MK-7246
CAS:1218918-62-7	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.
產(chǎn)品類別: 抑制劑
貨號(hào): TQ0051

Product Introduction

Bioactivity

名稱	MK-7246
描述	MK-7246 is a potent and specific CRTH2 antagonist (Ki: 2.5 nM).
激酶實(shí)驗(yàn)	The binding kinetics of [3H]MK-7246 (specific activity, 41 Ci/mmol) at human CRTH2 is characterized using recombinant HEK293E cell membranes. The radioligand binding experimental condition for CRTH2 as follows: the incubation mixture contains 10 mM MgCl2 instead of MnCl2, 10 nM [3H]MK-7246, and 1.25 μg of membrane protein. Total binding represents 10% of the radioligand adds to the incubation media, and specific binding at equilibrium corresponded to 85 to 95% of the total binding. The membranes are first incubated with [3H]MK-7246 for 120 min in the absence (total binding) or presence (nonspecific binding) of 10 μM MK-7246. To one series of total binding incubation tubes, 10 μM MK-7246 or 100 μM PGD2 is added to initiate dissociation of the radioligand from the receptor, and the reaction is left to proceed for up to 300 min. The samples are then harvested and processed as detailed above. The association and dissociation kinetic data analysis is done by nonlinear regression curve-fitting using Prism software to determine the observed on rate (Kobs) and dissociation rate (koff) constants, and t1/2 of on and off rates [1].
動(dòng)物實(shí)驗(yàn)	Intratracheal Budesonide is dosed 1 h prior to and 23 h post the A. alternate intratracheal dose while oral Budesonide (3 mg/kg) is administered 2 h before and 22 h post the A. alternata extract instillation. An intratracheally dosed Budesonide is prepared. MK-7246 (3, 10, 30 and 100 mg/kg) is administered orally 1 h before and 23 h post an A. alternata extract instillation in order to examine the effect of the CRTH2 antagonist on A. alternata elicited pulmonary inflammatory responses. Budesonide dosed orally is used as a positive control in both experiments. The animals are lightly anesthetized with 3% Isoflurane (supplemented with 100% oxygen), either 2 h following oral dosing or 1 h following intratracheal dosing. The animals are also secured on a rodent work stand to facilitate the localization of the larynx and tracheal openings. The micro sprayer needle is inserted into the trachea and 0.1 mL of 10,000 μg/mL (total of 1000 μg) A. alternata extract is administered using a micro sprayer. The animals are observed until they recover from anesthesia and then return to their cages and allow food and water ad libitum [2].
體外活性	MK-7246 competes for [3H]PGD2 specific binding to cell membranes expressing recombinant human CRTH2 with high-affinity (Ki, 2.5 nM). MK-7246 displays relatively high selectivity for CRTH2 with an affinity 149-fold lower for the DP receptor (Ki, 373±96 nM) and ≥1500-fold lower for the other prostanoid receptors (Ki, 7668±2169 nM for EP2, 3804±1290 nM for TP). MK-7246 is also tested in a panel of 157 enzyme and receptor assays at concentrations up to 100 μM and small but significant activity is detected only on phosphodiesterase 1 (PDE1, IC50=33.2 μM) and MAPK3 (ERK1, IC50=49.4 μM) [1].
體內(nèi)活性	Whether the inhibition of a clinically-relevant mechanism of allergic lung inflammation such as CRTH2 will lead to a suppression of inflammatory responses is investigated in A. alternata challenged Brown Norway rats (n=8 per group). CRTH2 inhibitor MK-7246 is orally administered 1 h before and 23 h post-intratracheal instillation of the A. alternata. MK-7246 produces a dose-dependent decrease in the number of eosinophils with a maximal inhibition of 74±5% in the 100 mg/kg group (P<0.05), IL-5 (80±12%) and IL-13 (76±14%) cytokines levels (P<0.05) [2].
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 : 245 mg/mL (588.27 mM)
關(guān)鍵字	MK7246 \| MK 7246 \| MK-7246
相關(guān)產(chǎn)品	Benzyl nicotinate \| CRTh2 antagonist 2 \| Ramatroban \| CAY10595 \| Questiomycin A \| TUG-1375 \| NF-56-EJ40 \| Monomethyl fumarate \| 3-Hydroxyoctanoic Acid \| Fezagepras sodium \| Timapiprant \| Vincamine

關(guān)鍵字： MK-7246|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(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。

成立日期	2013-04-18 （12年）	注冊(cè)資本	566.265100萬人民幣
員工人數(shù)	100-500人	年?duì)I業(yè)額	￥ 1億以上
主營行業(yè)	天然產(chǎn)物,生化試劑,分子生物學(xué),分子砌塊,生物技術(shù)服務(wù)	經(jīng)營模式	貿(mào)易,工廠,試劑,定制,服務(wù)

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公司成立：12年
注冊(cè)資本：566.265100萬人民幣
企業(yè)類型：有限責(zé)任公司(自然人投資或控股)
主營產(chǎn)品：小分子抑制劑、藥物篩選化合物庫、藥物篩選等
公司地址：靜安區(qū)江場三路238號(hào)8樓

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