Otaplimastat|1176758-04-5|(SP-8203)-陌孚医药/Medlife

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Otaplimastat (Synonyms: SP-8203)

目录号: PL07424 纯度: ≥98%

CAS No. :1176758-04-5

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中文名称	Otaplimastat
英文名称	Otaplimastat
英文别名	Otaplimastat;UYE03B60KA;3(2H)-yl)propyl]amino}butyl)acetamide;J3.046.690J;N-(4-{[3-(2,4-dioxo-1,4-dihydroquinazolin-;N-[3-(2,4-dioxo-1,4-dihydroquinazolin-3(2H)-yl)propyl]-;Acetamide, N-[3-(1,4-dihydro-2,4-dioxo-3(2H)-quinazolinyl)propyl]-N-[4-[[3-(1,4-dihydro-2,4-dioxo-3(2H)-quinazolinyl)propyl]amino]butyl]-;N-(3-(2,4-dioxo-1,4-dihydroquinazolin-3(2H)-yl)propyl)-N-(4-((3-(2,4-dioxo-1,4-dihydroquinazolin-3(2H)-yl)propyl)amino)butyl)acetamide;Acetamide, N-(3-(
Cas No.	1176758-04-5
分子式	C₂₈H₃₄N₆O₅
分子量	534.61
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Otaplimastat (SP-8203) 是一种基质金属蛋白酶 (MMP) 抑制剂，以竞争方式阻断 NMDA 受体介导的兴奋性毒性。Otaplimastat 还具有抗氧化活性。Otaplimastat 可用于脑缺血损伤的研究。

生物活性

Otaplimastat (SP-8203), a matrix metalloproteinase (MMP) inhibitor, blocks N-methyl-D-aspartate (NMDA) receptor-mediated excitotoxicity in a competitive manner. Otaplimastat also exhibits anti-oxidant activity. Otaplimastat can be used for the research of brain ischemic injury.

性状

Solid

IC50 & Target[1][2]

MMP NMDA

体外研究(In Vitro)

Otaplimastat (87.5-350 μM; 20 min) protects neuronal cells against NMDA-induced cell death in a competitive manner.
Otaplimastat (350 μM) inhibits Ca influx following activation of NMDA receptors in primary cultured neuron.
Otaplimastat (2-200 μM; pretreated for 4 h) significantly suppresses H2O2-induced cell death and reactive oxygen species production.
has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Otaplimastat (10-20 mg/kg; i.p. 30 min before occlusion and 1 h after reperfusion) prevents ischemic neuronal death in the occlusion model of MCA.
Otaplimastat (5-10 mg/kg; i.p. daily for 10 days) attenuates impairment of stroke-induced motor function. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Noh SJ, et, al. SP-8203 shows neuroprotective effects and improves cognitive impairment in ischemic brain injury through NMDA receptor. Pharmacol Biochem Behav. 2011 Nov;100(1):73-80.
[2]. Noh SJ, et, al. SP-8203 reduces oxidative stress via SOD activity and behavioral deficit in cerebral ischemia. Pharmacol Biochem Behav. 2011 Mar;98(1):150-4.

溶解度数据	In Vitro: DMSO : 100 mg/mL (187.05 mM; Need ultrasonic)配制储备液

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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