1176758-04-5

1176758-04-5 structure

Name: Otaplimastat
Chemical Name: SP-8203
CAS Number: 1176758-04-5
Molecular Formula: C₂₈H₃₄N₆O₅
Molecular Weight: 534.607
Catalog: Signaling Pathways Membrane Transporter/Ion Channel iGluR
Create Date: 2018-06-23 04:53:29
Modify Date: 2024-01-10 11:48:01
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].

Name	SP-8203
Synonyms	SP-8203 N-[3-(2,4-Dioxo-1,4-dihydro-3(2H)-quinazolinyl)propyl]-N-(4-{[3-(2,4-dioxo-1,4-dihydro-3(2H)-quinazolinyl)propyl]amino}butyl)acetamide UYE03B60KA 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]-

Description	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].
Related Catalog	Signaling Pathways >> Neuronal Signaling >> iGluR Signaling Pathways >> Metabolic Enzyme/Protease >> MMP Research Areas >> Neurological Disease Signaling Pathways >> Membrane Transporter/Ion Channel >> iGluR
Target	MMP NMDA
In Vitro	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].
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[1]. Otaplimastat (5-10 mg/kg; i.p. daily for 10 days) attenuates impairment of stroke-induced motor function[2]. Animal Model: Male Wistar rats (280-310 g, 9 weeks) were induced transient middle cerebral artery (MCA) occlusion[1] 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.
References	[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.

Density	1.3±0.1 g/cm3
Molecular Formula	C₂₈H₃₄N₆O₅
Molecular Weight	534.607
Exact Mass	534.259094
LogP	1.76
Index of Refraction	1.589

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