(-)-MK-801 maleate
(Synonyms: (-)-Dizocilpine Maleate) 目录号 : GC15270
(-)-MK 801是一种选择性、非竞争性N-甲基-D-天冬氨酸（NMDA）受体拮抗剂（Ki = 211.7nM）。
Cas No.:121917-57-5
Sample solution is provided at 25 µL, 10mM.
(-)-MK 801 is a selective, noncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist (Ki = 211.7nM) [1]. (-)-MK 801 inhibits calcium influx into cells by physically blocking calcium (Ca²⁺) channels in the open state of NMDA receptors activated by glutamate and glycine [2-3]. (-)-MK 801 has anticonvulsant and neuroprotective properties [4].
In Panc-1 cells, cell proliferation was significantly inhibited by 1000μM (-)-MK 801 (0.1-1000μM; 48h) [5]. In HepG2 cells, (-)-MK 801 (62.5-500μM; 72h) inhibits cancer cell growth [6].
In sprague dawley rats, after (-)-MK 801 (0.2mg/kg; ip; 10d) treatment, rats showed impaired performance in multiple sensorimotor tests and developed severe symptoms of intoxication [7]. In albino mice, high-dose (-)-MK 801 (10mg/kg; ip; 5 months) treatment kills a small number of PC/RS cortical neurons in mice, leading to chronic learning impairment in spatial learning [8].
References:
[1]. Yang B, Ren Q, Ma M, et al. Antidepressant effects of (+)-MK-801 and (-)-MK-801 in the social defeat stress model[J]. International Journal of Neuropsychopharmacology, 2016, 19(12): pyw080.
[2]. Decollogne S, Tomas A, Lecerf C, et al. NMDA receptor complex blockade by oral administration of magnesium: comparison with MK-801[J]. Pharmacology Biochemistry and Behavior, 1997, 58(1): 261-268.
[3]. Song X, Jensen M Ø, Jogini V, et al. Mechanism of NMDA receptor channel block by MK-801 and memantine[J]. Biophysical Journal, 2018, 114(3): 24a-25a.
[4]. Urbańska E, Dziki M, Kleinrok Z, et al. Influence of MK-801 on the anticonvulsant activity of antiepileptics[J]. European journal of pharmacology, 1991, 200(2-3): 277-282.
[5]. Malsy M, Gebhardt K, Gruber M, et al. Effects of ketamine, s-ketamine, and MK 801 on proliferation, apoptosis, and necrosis in pancreatic cancer cells[J]. BMC anesthesiology, 2015, 15(1): 111.
[6]. Yamaguchi F, Hirata Y, Akram H, et al. FOXO/TXNIP pathway is involved in the suppression of hepatocellular carcinoma growth by glutamate antagonist MK-801[J]. BMC cancer, 2013, 13(1): 468.
[7]. Wozniak D F, Olney J W, Kettinger III L, et al. Behavioral effects of MK-801 in the rat[J]. Psychopharmacology, 1990, 101(1): 47-56.
[8]. Wozniak D F, Brosnan-Watters G, Nardi A, et al. MK-801 neurotoxicity in male mice: histologic effects and chronic impairment in spatial learning[J]. Brain research, 1996, 707(2): 165-179.
(-)-MK 801是一种选择性、非竞争性N-甲基-D-天冬氨酸（NMDA）受体拮抗剂（Ki = 211.7nM） [1]。(-)-MK 801通过物理阻断谷氨酸和甘氨酸激活的NMDA受体开放状态下的钙（Ca²⁺）通道，抑制钙离子内流进入细胞 [2-3]。(-)-MK 801具有抗惊厥和神经保护作用 [4]。
在Panc-1细胞中，1000μM (-)-MK 801（0.1-1000μM；48h）显著抑制细胞增殖 [5]。在HepG2细胞中，(-)-MK 801（62.5-500μM；72h）可抑制癌细胞生长 [6]。
在Sprague-Dawley大鼠中，(-)-MK 801（0.2mg/kg；ip；10d）治疗后，大鼠在多项感觉运动测试中表现出表现受损，并出现严重的中毒症状 [7]。在白化小鼠中，高剂量(-)-MK 801（10mg/kg；ip；5个月）治疗会杀死小鼠少量PC/RS皮质神经元，导致空间学习能力出现慢性学习障碍 [8]。
| Cell experiment [1]: | |
Cell lines | Panc-1 cells |
Preparation Method | Cells were incubated with 100μL of the test compounds for 48h (0.1-1000μM ketamine, s-ketamine, and (-)-MK 801). After 32h incubation, cells were additionally treated with BrdU labeling solution for the last 16h. The culture medium was removed, cells were fixed, and DNA was denatured. Afterwards, cells were incubated with Anti-BrdU-POD solution for 90min, and antibody conjugates were removed in three washing cycles. Immune complexes were detected by means of TMB substrate for 15min and quantified by measuring the absorbance at 405nm and 490nm. |
Reaction Conditions | 0.1-1000μM; 48h |
Applications | In Panc-1 cells, cell proliferation was significantly inhibited by 1000μM (-)-MK 801. |
| Animal experiment [2]: | |
Animal models | Sprague dawley rats |
Preparation Method | (-)-MK 801 was dissolved in distilled water and adjusted to a neutral pH (7.3 +0.1) with NaOH. Drug challenge procedures commenced on day 31 and were carried out on every third day thereafter up to day 40. On day 31, five rats received injections of 0.2mg/kg (-)-MK 801 (injection volumes: 0.5mL) and five received saline. |
Dosage form | 0.2mg/kg; ip; 10d |
Applications | After (-)-MK 801 treatment, rats showed impaired performance in multiple sensorimotor tests and developed severe symptoms of intoxication. |
References: | |
| Cas No. | 121917-57-5 | SDF | |
| 别名 | (-)-Dizocilpine Maleate | ||
| Canonical SMILES | C[C@@]1(N2)C3=CC=CC=C3C[C@H]2C4=CC=CC=C14.O=C(O)/C=C\C(O)=O | ||
| 分子式 | C20H19NO4 | 分子量 | 337.37 |
| 溶解度 | ≥ 10.3mg/mL in DMSO | 储存条件 | 4°C, sealed storage, away from moisture |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9641 mL | 14.8205 mL | 29.641 mL |
| 5 mM | 0.5928 mL | 2.9641 mL | 5.9282 mL |
| 10 mM | 0.2964 mL | 1.4821 mL | 2.9641 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.00%
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