For research use only. Not for therapeutic Use.
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[1][2][3].
Otaplimastat (87.5-350 μM; 20 min) protects neuronal cells against NMDA-induced cell death in a competitive manner[1].
Otaplimastat (350 μM) inhibits Ca2+ influx following activation of NMDA receptors in primary cultured neuron[1].
Otaplimastat (2-200 μM; pretreated for 4 h) significantly suppresses H2O2-induced cell death and reactive oxygen species production[2].
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[1].
Otaplimastat (5-10 mg/kg; i.p. daily for 10 days) attenuates impairment of stroke-induced motor function[2].
| Catalog Number | I036525 |
| CAS Number | 1176758-04-5 |
| Synonyms | N-[3-(2,4-dioxo-1H-quinazolin-3-yl)propyl]-N-[4-[3-(2,4-dioxo-1H-quinazolin-3-yl)propylamino]butyl]acetamide |
| Molecular Formula | C28H34N6O5 |
| Purity | ≥95% |
| InChI | InChI=1S/C28H34N6O5/c1-20(35)32(17-9-19-34-26(37)22-11-3-5-13-24(22)31-28(34)39)16-7-6-14-29-15-8-18-33-25(36)21-10-2-4-12-23(21)30-27(33)38/h2-5,10-13,29H,6-9,14-19H2,1H3,(H,30,38)(H,31,39) |
| InChIKey | SJZBPVOSFYUHFV-UHFFFAOYSA-N |
| SMILES | CC(=O)N(CCCCNCCCN1C(=O)C2=CC=CC=C2NC1=O)CCCN3C(=O)C4=CC=CC=C4NC3=O |
| Reference | [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. [3]. Kim JS, et, al. Safety and Efficacy of Otaplimastat in Patients with Acute Ischemic Stroke Requiring tPA (SAFE-TPA): A Multicenter, Randomized, Double-Blind, Placebo-Controlled Phase 2 Study. Ann Neurol. 2020 Feb;87(2):233-245. |
