Cat. No.: HY-109097

Otaplimastat

(Synonyms: SP-8203)

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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.

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Pureté: 98.11%
CAS No.: 1176758-04-5
Formule: C₂₈H₃₄N₆O₅
Masse moléculaire:534.61

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Otaplimastat Chemical Structure

CAS No.: 1176758-04-5

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Stock

Quantité

Sample (0.1mg)

In-stock

(In Japan)

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Solvant et solubilité
- In Vitro
Pureté et documentation
Références
Help & FAQs
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

NMDA Receptor

MMP

Voir tous les produits spécifiques à Isoform MMP :

Voir tous les produits spécifiques à Isoform iGluR :

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.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1176758-04-5
Appearance Solid
Masse moléculaire 534.61
Formule C₂₈H₃₄N₆O₅
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
Synonyms

SP-8203
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvant et solubilité

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8705 mL

9.3526 mL

18.7052 mL

5 mM

0.3741 mL

1.8705 mL

3.7410 mL

10 mM

0.1871 mL

0.9353 mL

1.8705 mL

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (271 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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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Otaplimastat

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Voir tous les produits spécifiques à Isoform MMP

Voir tous les produits spécifiques à Isoform iGluR

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Otaplimastat Related Classifications

Cat. No.: HY-109097