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Merck
CN

475878

(+)-MK 801马来酸盐

A highly potent, selective, and non-competitive NMDA receptor antagonist that acts by binding to a site located within the NMDA-associated ion channel, thus preventing Ca2+ flux.

别名:

(+)-MK 801马来酸盐, (5R,10S)-(+)-5-甲基-10,11-二氢-5H-二苯并[a,d]-环庚-5-10-亚胺,马来酸盐,马来酸地佐西平,NMDA拮抗剂I

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关于此项目

经验公式(希尔记法):
C16H15N · xC4H4O4
化学文摘社编号:
分子量:
221.30 (free base basis)
UNSPSC Code:
12352200
MDL number:
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InChI

1S/C16H15N.C4H4O4/c1-16-13-8-4-2-6-11(13)10-15(17-16)12-7-3-5-9-14(12)16;5-3(6)1-2-4(7)8/h2-9,15,17H,10H2,1H3;1-2H,(H,5,6)(H,7,8)/b;2-1-/t15-,16+;/m1./s1

InChI key

QLTXKCWMEZIHBJ-PJGJYSAQSA-N

assay

≥98% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, desiccated

color

white

solubility

water: 3 mg/mL, ethanol: soluble

shipped in

ambient

Quality Level

General description

一种高效,选择性和非竞争性NMDA受体拮抗剂,通过与位于NMDA相关离子通道内的位点结合而起作用,从而防止Ca2+通量。几种动物模型中的有效抗缺血剂。已被用于在发育中的大鼠脑中开发NMDA受体依赖性凋亡性神经退行性疾病的体内模型。还已用于开发NMDA受体特异性Ca2+进入诱导的癫癇发作的体外模型。
一种高效,选择性和非竞争性NMDA受体拮抗剂,通过与位于NMDA相关离子通道内的位点结合而起作用,防止Ca2+通量。几种动物模型中的有效抗缺血剂。已被用于在发育中的大鼠脑中开发NMDA受体依赖性凋亡性神经退行性疾病的体内模型。还已用于开发NMDA受体特异性Ca2+进入诱导的癫癇发作的体外模型。

Biochem/physiol Actions

主要靶标
NMDA受体
可逆:否
细胞渗透性:否

Preparation Note

在水中复溶后,冷藏(4°C)短期储存或等分和冷冻(-20°C)进行长期储存。贮备水溶液在4°C下可稳定保存长达 1 个月,在-20°C下可稳定保存长达 3 个月。
水中的贮备液可能需要加热并剧烈搅拌才能完全溶解。

Other Notes

Ikonomidou, C., et al. 1999.Science 283, 70.
DeLorenzo, R.J., et al. 1998.Proc.Natl.Acad.Sci. USA 95, 14482.
Woodruff, G.N., et al. 1987.Neuropharmacology 26, 903.
Wong, E.H.F., et al. 1986.Proc.Natl.Acad.Sci. USA 83, 7104.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

毒性:标准处理(A)

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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Glutamate is an excitatory neurotransmitter found in the synaptic vesicles of glutamatergic synapses. The post-synaptic neurons in these synapses contain ionotropic and metabotropic glutamate receptors. Glutamate binds to AMPA (α-amino-3-hydroxy-5- methylisoxazole-4-propionic acid) subtype glutamate receptors, leading to sodium influx into the post-synaptic cell and resulting in neuronal excitability and synaptic transmission. The NMDA (N-methyl-d-aspartate) subtype glutamate receptors, on the other hand, regulate synaptic plasticity, and can influence learning and memory. The metabotropic g-protein coupled mGluRs modulate downstream calcium signaling pathways and indirectly influence the synapse’s excitability. The synaptic architecture includes intracellular scaffolding proteins (PSD-95, GRIP), intercellular cell adhesion molecules (NCAMs, N-Cadherins), and a variety of signaling proteins (CaMKII/PKA, PP1/PP2B). Processes critical for synaptic transmission and plasticity are influenced by these molecules and their interactions. When the function of these molecules is disrupted, it leads to synaptic dysfunction and degeneration, and can contribute to dementia as seen in Alzheimer’s disease.

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