SDZ 220-581 hydrochloride
(Synonyms: (S)-ALPHA-氨基-2'-氯-5-(膦酰甲基)-[1,1'-联苯]-3-丙酸盐酸盐) 目录号 : GC16986SDZ 220-581 hydrochloride 是一种口服有效的竞争性 NMDA 受体拮抗剂,pKi 值为 7.7。
Cas No.:179411-93-9
Sample solution is provided at 25 µL, 10mM.
SDZ 220-581 hydrochloride is a potent and competitive antagonist of NMDA receptor with pKi value of 7.7 [1].
SDZ 220-581 is a biphenyl-AP7-derivative. It is potent both in vitro and in vivo. SDZ 220-581 binds with high affinity to the recognition site of NMDA receptor. It does not bind to the strychnine-insensitive glycine site or the MK-801 site within the NMDA receptor. In addition, SDZ 220-581 shows no effect on a variety of other binding assays such as for dopamine, serotonin and adenosine [1].
In the in vivo assay, the administration of SDZ 220-581 protects the mice against the maximal electroshock-induced seizures (MES). In the rat MES model, SDZ 220-581 also shows potent efficacy. Moreover, SDZ 220-581 can protect brain against quinolinic acid induced neuronal degeneration in rat. Furthermore, a dose of 1.25mg/kg SDZ 220-581 markedly reduces the cerebral infarct size in the focal cerebral ischemia model in rat [2].
References:
[1] Urwyler et al .Biphenyl-derivatives of 2-amino-7-phosphono-heptanoic acid, a novel class of potent competitive N-methyl-D-aspartate receptor antagonists - II. Pharmacological characterization in vivo. Neuropharmacology 1996, 35 655.
[2] Urwyler S, Campbell E, Fricker G, et al. Biphenyl-derivatives of 2-amino-7-phosphono-heptanoic acid, a novel class of potent competitiveN-Methyl-D-aspartate receptor antagonists—II. Pharmacological characterization in vivo[J]. Neuropharmacology, 1996, 35(6): 655-669.
Cas No. | 179411-93-9 | SDF | |
别名 | (S)-ALPHA-氨基-2'-氯-5-(膦酰甲基)-[1,1'-联苯]-3-丙酸盐酸盐 | ||
化学名 | (S)-2-amino-3-(2'-chloro-5-(phosphonomethyl)-[1,1'-biphenyl]-3-yl)propanoic acid hydrochloride | ||
Canonical SMILES | ClC1=CC=CC=C1C2=CC(C[C@@](N)([H])C(O)=O)=CC(CP(O)(O)=O)=C2.Cl | ||
分子式 | C16H18Cl2NO5P | 分子量 | 406.2 |
溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
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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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.4618 mL | 12.3092 mL | 24.6184 mL |
5 mM | 0.4924 mL | 2.4618 mL | 4.9237 mL |
10 mM | 0.2462 mL | 1.2309 mL | 2.4618 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 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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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,
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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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- Purity: >99.50%
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