SNJ-1945
Based on 1 Customer Validation
SNJ-1945 is an orally active, blood-brain barrier-penetrant Calpain inhibitor. SNJ-1945 inhibits Cathepsin L, Cathepsin B, and Ca2+ -independent proteases. SNJ-1945 suppresses ROS production and downregulates Cyclooxygenase-2 and Caspase-1. SNJ-1945 alleviates left ventricular systolic dysfunction, reduces cerebral ischemia-induced injury, and decreases the score of experimental autoimmune encephalomyelitis in mouse models. SNJ-1945 can be used in research related to post-cardiac arrest reperfusion injury, Parkinson's disease, multiple sclerosis, and proliferative retinopathy.
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- Pureté : 99.49%
- CAS No.: 854402-59-8
- Formule: C25H37N3O7
- Masse moléculaire:491.58
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[2]|
Caspase-1 |
COX-2 |
Cathepsin B |
cathepsin L |
In Vitro
SNJ-1945 (100-250 μM) protects dopaminergic SH-SY5Y-DA cells and cholinergic SH-SY5Y-ChAT cells against viability loss and apoptotic morphological changes induced by 1-methyl-4-phenylpyridinium ion and Rotenone (HY-B1756); partial protective effects are achieved when it is administered 1-3 h after exposure to the neurotoxicants[2].
SNJ-1945 (250 μM) reduces reactive oxygen species production induced by MPP+ and Rotenone in dopaminergic SH-SY5Y-DA cells[2].
SNJ-1945 (50-250 μM) dose-dependently attenuates the increased expression of cyclooxygenase-2, caspase-1, and the activated caspase-1 p10 fragment induced by MPP+ and rotenone in cholinergic SH-SY5Y-ChAT cells[2].
SNJ-1945 (250 μM; 30 min) does not inhibit VEGF-induced calcium uptake in cultured retinal microvascular endothelial cells[4].
SNJ-1945 (100-250 μM; 48 h) inhibits VEGF-induced migration of cultured retinal microvascular endothelial cells in vitro in a dose-dependent manner[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Differentiated SH-SY5Y human neuroblastoma cells (dopaminergic SH-SY5Y-DA and cholinergic SH-SY5Y-ChAT phenotypes)
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Concentration:10-250 μM (pre-treated 30 min prior to neurotoxicant exposure); 50-250 μM (administered 1-3 h post-neurotoxicant exposure)
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Incubation Time:24 h (total incubation with neurotoxicant)
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Result:Exhibited no overt effect on cell viability at 250 μM alone.
Significantly protected SH-SY5Y-DA and SH-SY5Y-ChAT cells against 1-methyl-4-phenylpyridinium and rotenone-induced loss of cell viability at 100 and 250 μM.
Dose-dependently ameliorated the apoptotic morphological alterations (deeply stained, shrunken nuclei) induced by 1-methyl-4-phenylpyridinium or rotenone in both cell phenotypes when pre-treated.
Provided partial protection to cells when administered 1-3 h after neurotoxicant exposure.
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Cell Line:human retinal microvascular endothelial cells (HRMEC)
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Concentration:100-250 μM
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Incubation Time:48 h
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Result:Blocked VEGF-induced HRMEC migration in a dose-dependent manner, reducing the repaired wound area compared to VEGF alone.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:B10.PL (male, 4-5 weeks old, 18-20 grams, EAE induced via subcutaneous immunization with guinea pig MBP in CFA plus pertussis toxin injection)[3]
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Dosage:50 mg/kg
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Administration:p.o.; twice daily; from day 9 post-induction until sacrifice
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Result:Reduced EAE paralysis scores and delayed the peak of paralytic signs relative to vehicle-treated EAE mice.
Reduced antigen-stimulated proliferation in lymph node cells.
Decreased inflammatory IL-17 cytokine levels and increased anti-inflammatory IL-10 cytokine levels in lymph node cells.
Increased the number of cells expressing IL-4 and STAT6, myeloid-derived suppressor cells, and IL-5-expressing cells in peripheral blood mononuclear cells.
Decreased CCR6-expressing inflammatory Th17 cells and increased CD25-positive regulatory T cells in lymph nodes.
Decreased IL-17 mRNA expression and increased FoxP3 mRNA expression in splenocytes.
Reduced calpain protein expression, immune cell infiltration and perivascular cuffing, GFAP-positive gliosis, CD11b-positive microgliosis, dephosphorylated neurofilament protein, and TUNEL-positive neuronal cell death in spinal cords.
Preserved myelin surrounding axons in spinal cords.
Chemical Information
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CAS No. 854402-59-8
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Appearance Solid
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Masse moléculaire 491.58
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Formule C25H37N3O7
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Color White to off-white
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SMILES
O=C(C(NC1CC1)=O)[C@@H](NC([C@H](CC(C)C)NC(OCCOCCOC)=O)=O)CC2=CC=CC=C2
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Livraison
Room temperature in continental US; may vary elsewhere.
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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 : 50 mg/mL (101.71 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (289 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)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Yoshikawa Y, et al. Cardioprotective effects of a novel calpain inhibitor SNJ-1945 for reperfusion injury after cardioplegic cardiac arrest. American journal of physiology. Heart and circulatory physiology. 2010 Feb;298(2):H643-51. [Content Brief]
[2]. Knaryan VH, et al. SNJ-1945, a calpain inhibitor, protects SH-SY5Y cells against MPP(+) and rotenone. Journal of neurochemistry. 2014 Jul;130(2):280-90. [Content Brief]
[3]. Trager N, et al. Effects of a novel orally administered calpain inhibitor SNJ-1945 on immunomodulation and neurodegeneration in a murine model of multiple sclerosis. Journal of neurochemistry. 2014 Jul;130(2):268-79. [Content Brief]
[4]. Ma H, et al. Calpain inhibitor SNJ-1945 attenuates events prior to angiogenesis in cultured human retinal endothelial cells. Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics. 2009 Oct;25(5):409-14. [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 |
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| DMSO | 1 mM | 2.0343 mL | 10.1713 mL | 20.3426 mL | 50.8564 mL |
| 5 mM | 0.4069 mL | 2.0343 mL | 4.0685 mL | 10.1713 mL | |
| 10 mM | 0.2034 mL | 1.0171 mL | 2.0343 mL | 5.0856 mL | |
| 15 mM | 0.1356 mL | 0.6781 mL | 1.3562 mL | 3.3904 mL | |
| 20 mM | 0.1017 mL | 0.5086 mL | 1.0171 mL | 2.5428 mL | |
| 25 mM | 0.0814 mL | 0.4069 mL | 0.8137 mL | 2.0343 mL | |
| 30 mM | 0.0678 mL | 0.3390 mL | 0.6781 mL | 1.6952 mL | |
| 40 mM | 0.0509 mL | 0.2543 mL | 0.5086 mL | 1.2714 mL | |
| 50 mM | 0.0407 mL | 0.2034 mL | 0.4069 mL | 1.0171 mL | |
| 60 mM | 0.0339 mL | 0.1695 mL | 0.3390 mL | 0.8476 mL | |
| 80 mM | 0.0254 mL | 0.1271 mL | 0.2543 mL | 0.6357 mL | |
| 100 mM | 0.0203 mL | 0.1017 mL | 0.2034 mL | 0.5086 mL |
SNJ-1945 Related Classifications
HY-136903 Related Classifications
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