L-689,560
目录号 : GC10696
L-689,560 是一种有效的 N-甲基-D-天冬氨酸 (NMDA) 受体拮抗剂，作用于 GluN1 甘氨酸结合位点。
Cas No.:139051-78-8
Sample solution is provided at 25 µL, 10mM.
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Kb: 130 nM
L-689,560 is a very potent antagonist at the glycine-NMDA site. The N-methyl-D-aspartate (NMDA) subtype of excitatorynamino acid receptor has been proved adequately that its relevant antagonists can reduce ischaemic brain damage (particularly in experimental models of focal cerebral ischaemia).
In vitro: L-689560 is described as one of the most potent NMDA antagonists and [4'-3H]-L-689560 has been thought to be a highly specific radioligand for the glycine site. In consistent with the 5,7-disubstituted kynurenates, the tetrahydroquinolines are selective antagonists of glycine site NMDA, L-689560 exhibiting at least 3 orders of magnitude selectivity versus the glutamate site [1].
In vivo: MDL100748 with an ED50 of 83 mg kg-1 can prevent audiogenic seizures in susceptible mice after systemic injection. As a standard L689560, its subsequent analogues have been compared; the displacement of [3H] L689560 has often been used to displace that of [3H] glycine as an alternative assay. L701252, a quinones (the retention of a keto grouping at position 3), has been against L689560 binding (IC50 of 420 nM) and against seizures (ED50 of 4.1 mg kg-1) in DBA/2 mice. A group of sulfonamide analogues of kynurenic acid are also in active among the 2-quinolone series. Those of a series of 3,4-dihydroquinolones and tetrahydroquinolines with a nitrosubstituent at 3-position were selective antagonists at the NMDA receptor glycine site if they bore a bulky grouping in the position 4. The compound with no substitution at position 4 was proved to be one of the most effective broad-spectrum antagonists against NMDA and AMPA receptors [2].
Clinical trial: So far, no clinical study has been conducted.
References:
[1]. Leeson PD, Carling RW, Moore KW, Moseley AM, Smith JD, Stevenson G, Chan T, Baker R, Foster AC, Grimwood S, et al. 4-Amido-2-carboxytetrahydroquinolines. Structure-activity relationships for antagonism at the glycine site of the NMDA receptor. J Med Chem. 1992 May 29;35 (11): 1954-68.
[2]. Stone TW. Development and therapeutic potential of kynurenic acid and kynurenine derivatives for neuroprotection. Trends Pharmacol Sci. 2000 Apr; 21(4):149-54.
| Cas No. | 139051-78-8 | SDF | |
| 化学名 | (2S,4S)-5,7-dichloro-4-(3-phenylureido)-1,2,3,4-tetrahydroquinoline-2-carboxylic acid | ||
| Canonical SMILES | ClC1=C2[C@H](C[C@@H](C(O)=O)NC2=CC(Cl)=C1)NC(NC3=CC=CC=C3)=O | ||
| 分子式 | C17H15Cl2N3O3 | 分子量 | 380.23 |
| 溶解度 | <9.51mg/ml in DMSO; <38.02mg/ml in ethanol | 储存条件 | Store at RT |
| 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 | 2.63 mL | 13.1499 mL | 26.2999 mL |
| 5 mM | 0.526 mL | 2.63 mL | 5.26 mL |
| 10 mM | 0.263 mL | 1.315 mL | 2.63 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet