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编 号:F056146
分子式:C28H34N6O5
分子量:534.61
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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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.

体内研究:
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.Animal Model:Male Wistar rats (280-310 g, 9 weeks) were induced transient middle cerebral artery (MCA) occlusion
Dosage:10, 20 mg/kg
Administration:I.p. before 30 min and after an hour of the MCA-occlusion operation
Result:Significantly reduced infarct volume.Improved spatial learning and memory impairments.

体外研究:
Otaplimastat (87.5-350 μM; 20 min) protects neuronal cells against NMDA-induced cell death in a competitive manner.Otaplimastat (350 μM) inhibits Ca2+ 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.
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