(-)-MK 801馬來酸|T6352|TargetMol

價(jià)格	￥239	￥373	￥695
包裝	5mg	10mg	25mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-09-23

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產(chǎn)品詳情

中文名稱:(-)-MK 801馬來酸	英文名稱:(-)-Dizocilpine maleate
CAS:121917-57-5	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: 99.89%	產(chǎn)品類別: 抑制劑
貨號(hào): T6352

Product Introduction

Bioactivity

名稱	(-)-Dizocilpine maleate
描述	(-)-Dizocilpine maleate ((-)-MK 801 (Maleate)) is a potent, selective and non-competitive NMDA receptor antagonist with Kd of 37.2 nM in rat brain membranes.
細(xì)胞實(shí)驗(yàn)	Cell lines: mixed neuronal/glial cell culturesConcentrations: 10 μMIncubation Time: 30 minutesMethod: Primary mixed neuronal/glial cultures are prepared from fetal rat brains. Mature cultures are exposed to dissolved isoflurane [0.4 mM (1.8 minimum alveolar concentration) or 1.6 mM (7 minimum alveolar concentration)] or dizocilpine (10 μM), and NMDA (0 or 3 μM) at 37 ℃ for 30 minutes. Apoptosis is assessed using terminal-deoxy-nucleotidyl end-nick labeling oligonucleosomal DNA fragmentation enzyme-linked immunosorbent assay, and caspases-3 and -9 activation assays.
激酶實(shí)驗(yàn)	In vitro binding assays:For in vitro binding assays, cerebral cortices from male Sprague-Dawley rats (200-300 g) are homogenized in 9 volumes of ice-cold sucrose by nine strokes with a Teflon/glass homogenizer at 500 rpm. The homogenate is centrifuged for 10 min at 1000 x g, and the supernatant is recentrifuged at 10,000 x g for 20 min at 4 ℃. The pellet is suspended in assay buffer and incubated for 20 min prior to final centrifugation at 10,000 x g for 20 min at 4 ℃. The pellet is resuspended in assay buffer (70 ml per gram of original tissue). Binding of [3H] dizocilpine is measured by incubating 750 ul duplicate aliquots of this crude membrane suspension (=0.75 mg of protein) with 100 ul of buffer containing displacer or of buffer alone (total binding), 100 ul of 50 nM [3H] dizocilpine, and 50 ul of buffer for 60 min at 23 ℃. Nonspecific binding is defined by unlabeled dizocilpine. Incubation is terminated by rapid filtration through Whatman GF/B filters, which are washed immediately with two 5-ml portions of ice-cold assay buffer in a Brandel M 24-R cell harvester. The time required for the complete filtration and washing procedure is less than 10 sec. Radioactivity on the filters is determined by liquid scintillation counting in standard vials with 10 ml of Hydrofluor at 41% counting efficiency.
動(dòng)物實(shí)驗(yàn)	Animal Models: ischemic spinal cord injury medelFormulation: N/ADosages: 1 mg/kgAdministration: IV
體外活性	在體外神經(jīng)生理學(xué)研究中，使用大鼠皮層切片進(jìn)行的試驗(yàn)表明，dizocilpine對(duì)N-Me-D-Asp引起的去極化反應(yīng)顯示出強(qiáng)大、選擇性且非競(jìng)爭(zhēng)性的拮抗作用，但對(duì)kainate或quisqualate無效。phencyclidine、ketamine、SKF 10047及dizocilpine的對(duì)映體作為N-Me-D-Asp拮抗劑的效力與它們作為[3H]dizocilpine結(jié)合抑制劑的效力密切相關(guān)（r = 0.99）。這暗示dizocilpine的結(jié)合位點(diǎn)與N-Me-D-Asp受體相關(guān)聯(lián)，并為dizocilpine作為抗驚厥化合物的作用機(jī)制提供了解釋。
體內(nèi)活性	所有對(duì)照組大鼠在缺血性脊髓損傷(ISCI)后呈現(xiàn)嚴(yán)重的永久性神經(jīng)功能缺陷，而經(jīng)dizocilpine處理的大鼠在神經(jīng)功能結(jié)果上具有統(tǒng)計(jì)學(xué)意義上的改善(P < .05)并顯示良好恢復(fù)。組織病理學(xué)揭示，對(duì)照組大鼠腰段灰質(zhì)中出現(xiàn)嚴(yán)重的神經(jīng)元壞死，而dizocilpine處理的大鼠則顯示輕微損傷。這些結(jié)果證明，ISCI前給予單劑量dizocilpine可以提供顯著的神經(jīng)保護(hù)作用。
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	Ethanol : 7 mg/mL (20.7 mM) DMSO : 68 mg/mL (201.55 mM)
關(guān)鍵字	less-active \| transporters \| ()Dizocilpine maleate \| C 13737 \| Inhibitor \| Dizocilpine \| inhibit \| NMDA \| ( ) Dizocilpine maleate \| MK-801 Maleate \| C-13737 \| MK801 \| monoamine \| Ionotropic glutamate receptors \| iGluR \| Dizocilpine Maleate \| antidepressant \| MK-801 \| MK801 Maleate \| MK 801 \| MK 801 Maleate
相關(guān)產(chǎn)品	glycine \| L-Glutamic acid \| L-Glutamic acid monosodium salt
相關(guān)庫	抑制劑庫 \| 經(jīng)典已知活性庫 \| 已知活性化合物庫 \| 神經(jīng)遞質(zhì)受體化合物庫 \| 離子通道庫 \| 神經(jīng)退行性疾病化合物庫 \| 膜蛋白靶向化合物庫 \| 疼痛相關(guān)化合物庫

關(guān)鍵字： C13737|||(-)-MK 801 (Maleate)|||(-)-MK 801馬來酸|||(-)-MK 801 Maleate|TargetMol

公司簡(jiǎn)介

上海陶術(shù)生物科技有限公司為美國(guó)Target Molecule Corp. ( Target Mol ) 在上海建立的全資子公司。我們與美國(guó)波士頓、德國(guó)慕尼黑的同事一起，為北美、歐洲和亞洲從事藥物研發(fā)和生物學(xué)研究的科學(xué)家提供優(yōu)質(zhì)的產(chǎn)品和專業(yè)的服務(wù)。公司下設(shè)篩選事業(yè)部，化學(xué)事業(yè)部，生物事業(yè)部和新材料部。從虛擬篩選到實(shí)體化合物分子供應(yīng)；從商業(yè)化產(chǎn)品銷售到個(gè)性化定制合成；從對(duì)明確靶點(diǎn)的分子篩選到對(duì)明確分子的多靶點(diǎn)篩選，從高通量篩選到化學(xué)結(jié)構(gòu)優(yōu)化，我們都可以滿足您的科研用品及技術(shù)服務(wù)的需求。經(jīng)過在中國(guó)市場(chǎng)五年的精心耕耘，我們已成為篩選化合物領(lǐng)域優(yōu)秀的供應(yīng)商，為超過五百家學(xué)校和各類企業(yè)提供了品質(zhì)卓越的小分子化合物和藥物篩

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員工人數(shù)	100-500人	年?duì)I業(yè)額	￥ 1億以上
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公司成立：12年
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