Otaplimastat
Based on 1 Customer Validation
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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.11%
- CAS 番号: 1176758-04-5
- 分子式: C28H34N6O5
- 分子量:534.61
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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生物活性
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NMDA Receptor |
MMP |
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.
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.
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Animal Model:Male Wistar rats (280-310 g, 9 weeks) were induced transient middle cerebral artery (MCA) occlusion[1]
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Dosage:10, 20 mg/kg
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Administration:I.p. before 30 min and after an hour of the MCA-occlusion operation
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Result:Significantly reduced infarct volume.
Improved spatial learning and memory impairments.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1176758-04-5
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性状 Solid
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分子量 534.61
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分子式 C28H34N6O5
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Color Off-white to light yellow
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SMILES
CC(N(CCCN1C(NC2=C(C=CC=C2)C1=O)=O)CCCCNCCCN3C(NC4=C(C=CC=C4)C3=O)=O)=O
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別名
SP-8203
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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.
Working solution concentration: 0.22 mg/mL
純度とドキュメンテーション
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データシート (271 KB)
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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)
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取扱説明書 (2659 KB)
参考文献
[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]
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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