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MK-801
CAS No. 77086-21-6
MK-801 ( Dizocilpine )
产品货号. M15913 CAS No. 77086-21-6
MK-801 (Dizocilpine) 是一种有效的 N-甲基-D-天冬氨酸 (NMDA) 受体拮抗剂，Ki 为 30.5 nM。
纯度: >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| 规格 | 价格/人民币 | 库存 | 数量 |
| 5MG | ￥462 | 有现货 |
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| 10MG | ￥705 | 有现货 |
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| 25MG | ￥1239 | 有现货 |
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| 50MG | ￥2041 | 有现货 |
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| 100MG | ￥3281 | 有现货 |
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| 200MG | 获取报价 | 有现货 |
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| 500MG | 获取报价 | 有现货 |
|
| 1G | 获取报价 | 有现货 |
|
生物学信息
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产品名称MK-801
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注意事项本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
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产品简述MK-801 (Dizocilpine) 是一种有效的 N-甲基-D-天冬氨酸 (NMDA) 受体拮抗剂，Ki 为 30.5 nM。
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产品描述MK-801 (Dizocilpine) is a potent N-methyl-D-aspartate (NMDA) receptor antagonist with Ki of 30.5 nM.(In Vitro):Dizocilpine (MK-801) progressively suppresses of current induced by NMDA. Mg2+ (10 mM) prevents Dizocilpine from blocking the N-Me-D-Asp-induced current, even when Dizocilpine is applied for a long time in the presence of NMDA. Dizocilpine blocks NMDA-activated single-channel activity in outside-out patches.Dizocilpine (MK-801; <500 μM) inhibits activation of microglia induced by LPS with increased Cox-2 protein expression in BV-2 cells. Dizocilpine (<500 μM) reduces microglial TNF-α output with an EC50 of 400 μM in BV-2 cells.(In Vivo):Dizocilpine (MK 801) (1 mg/kg) treatment before each METH injection reduces the extent of DA depletion by 55% in striatal of mice. Dizocilpine (MK 801) (1 mg/kg) also attenuates the effects of METH on microglial activation in striatal of mice.Dizocilpine ((+)-MK 801) (0.05, 0.2 mg/kg, i.p.) attenuates subsequent cocaine-primed reinstatement without disruption in rats. Dizocilpine (MK 801) (0.2 mg/kg, i.p.) prior to two reactivation sessions in the home cage shows no suppression on subsequent cocaine-primed reinstatement.
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体外实验Dizocilpine (MK-801) progressively suppresses of current induced by NMDA. Mg2+ (10 mM) prevents Dizocilpine from blocking the N-Me-D-Asp-induced current, even when Dizocilpine is applied for a long time in the presence of NMDA. Dizocilpine blocks NMDA-activated single-channel activity in outside-out patches. Dizocilpine (MK-801; <500 μM) inhibits activation of microglia induced by LPS with increased Cox-2 protein expression in BV-2 cells. Dizocilpine (<500 μM) reduces microglial TNF-α output with an EC50 of 400 μM in BV-2 cells.
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体内实验Dizocilpine (MK 801) (1 mg/kg) treatment before each METH injection reduces the extent of DA depletion by 55% in striatal of mice. Dizocilpine (MK 801) (1 mg/kg) also attenuates the effects of METH on microglial activation in striatal of mice.Dizocilpine ((+)-MK 801) (0.05, 0.2 mg/kg, i.p.) attenuates subsequent cocaine-primed reinstatement without disruption in rats. Dizocilpine (MK 801) (0.2 mg/kg, i.p.) prior to two reactivation sessions in the home cage shows no suppression on subsequent cocaine-primed reinstatement.
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同义词Dizocilpine
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通路Membrane Transporter/Ion Channel
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靶点NMDAR
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受体NMDA Receptor
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研究领域Other Indications
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适应症——
化学信息
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CAS Number77086-21-6
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分子量221.3
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分子式C16H15N
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纯度>98% (HPLC)
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溶解度DMSO:67 mg/mL (302.75 mM);Ethanol:7 mg/mL (31.63 mM);Water:<1 mg/mL
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SMILESC[C@@]12C3=CC=CC=C3C[C@@H](N1)C4=CC=CC=C24
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化学全称——
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
1.Anderson P, Christy M E, Evans B E. 5-Alkyl or hydroxyalkyl substituted-10,11-dihydro-5H-dibenzoa,dcyclohepten-5,10-imines and anticonvulsant use thereof: US, US4399141P. 1983.
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