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

Otaplimastat  (Synonyms: SP-8203)

Cat. No.: HY-109097 Purity: 98.41%
COA 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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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 330 In-stock
Solution
10 mM * 1 mL in DMSO USD 330 In-stock
Solid
5 mg USD 300 In-stock
10 mg USD 480 In-stock
25 mg USD 950 In-stock
50 mg USD 1450 In-stock
100 mg USD 2250 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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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].

MedChemExpress (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].

MedChemExpress (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.
Clinical Trial
Molecular Weight

534.61

Formula

C28H34N6O5

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

CC(N(CCCN1C(NC2=C(C=CC=C2)C1=O)=O)CCCCNCCCN3C(NC4=C(C=CC=C4)C3=O)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (187.05 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8705 mL 9.3526 mL 18.7052 mL
5 mM 0.3741 mL 1.8705 mL 3.7410 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8705 mL 9.3526 mL 18.7052 mL 46.7631 mL
5 mM 0.3741 mL 1.8705 mL 3.7410 mL 9.3526 mL
10 mM 0.1871 mL 0.9353 mL 1.8705 mL 4.6763 mL
15 mM 0.1247 mL 0.6235 mL 1.2470 mL 3.1175 mL
20 mM 0.0935 mL 0.4676 mL 0.9353 mL 2.3382 mL
25 mM 0.0748 mL 0.3741 mL 0.7482 mL 1.8705 mL
30 mM 0.0624 mL 0.3118 mL 0.6235 mL 1.5588 mL
40 mM 0.0468 mL 0.2338 mL 0.4676 mL 1.1691 mL
50 mM 0.0374 mL 0.1871 mL 0.3741 mL 0.9353 mL
60 mM 0.0312 mL 0.1559 mL 0.3118 mL 0.7794 mL
80 mM 0.0234 mL 0.1169 mL 0.2338 mL 0.5845 mL
100 mM 0.0187 mL 0.0935 mL 0.1871 mL 0.4676 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Otaplimastat
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HY-109097
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