1. Metabolic Enzyme/Protease
    Neuronal Signaling
    Membrane Transporter/Ion Channel
  2. MMP
    iGluR
  3. Otaplimastat

Otaplimastat (Synonyms: SP-8203)

Cat. No.: HY-109097
Handling Instructions

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.

For research use only. We do not sell to patients.

Otaplimastat Chemical Structure

Otaplimastat Chemical Structure

CAS No. : 1176758-04-5

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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].

IC50 & Target[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

534.61

Formula

C₂₈H₃₄N₆O₅

CAS No.
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Otaplimastat
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HY-109097
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