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| 5mg |
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| 10mg |
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| 25mg |
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Purity: ≥98%
| Targets |
Edonerpic targets amyloid-β peptides (Aβ). It protects neurons against mitochondrial dysfunction and apoptosis. The compound's neurotrophic and neuroprotective effects suggest it may modulate pathways involved in neuronal survival and function. Its mechanism may involve inhibition of Aβ-induced neurotoxicity and preservation of mitochondrial function.
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| ln Vitro |
In the presence of Aβ, therapy with edonerpic maleate (T-817MA) maintains cortical neurons (1-42). Neuronal mortality caused by oxidative stress was avoided by a 24-hour pretreatment and sustained administration of 0.1 and 1 μM Edonerpic maleate. At 0.1 and 1 μM, edonerpic maleate virtually entirely inhibits GSH reduction. Comparing hippocampal slices treated with 1 μM edonerpic maleate to control slices, the former generated longer and more neurites. Significant increases in neurite length are observed at 0.1 and 1 μM for edonerpic maleate [1].
In vitro, edonerpic protects against sodium nitroprusside-induced mitochondrial dysfunction and apoptosis in primary rat cortical neurons at concentrations of 0.1 and 1 µM. It inhibits amyloid-β peptides (Aβ). These activities demonstrate its neuroprotective potential. The compound's effects on neuronal survival and function have been characterized in cell-based assays. |
| ln Vivo |
Post hoc testing showed that the average density of PSA-positive cells in the vehicle group and Aβ infusion + high-dose Edonerpic maleate (T-817MA) group was considerably greater than that in the Aβ infusion control group (P<0.01). The outcomes demonstrated that both the vehicle and Aβ infusion + high-dose Edonerpic maleate groups demonstrated robust neurogenesis and effective learning in a place learning task (PLT). Treatment with Edonerpic maleate and donepezil did not increase the average density of normal granulosa cells; Aβ infusion control group, Aβ infusion + high-dose Edonerpic maleate group, Aβ infusion + low-dose Edonerpic maleate group There was no significant difference in the average granule cell density between the Aβ infusion + donepezil group [2].
In vivo, edonerpic (8.4 mg/kg per day) has been studied for its neuroprotective effects. As a neurotrophic agent, it may have potential for the treatment of neurodegenerative diseases. The compound's ability to inhibit Aβ and protect neurons suggests potential for Alzheimer's disease research. Further preclinical studies would evaluate its efficacy in animal models. |
| Enzyme Assay |
In vitro receptor binding assays for edonerpic are not typically performed, as it is not a direct receptor antagonist. Instead, neuroprotective assays are used. Primary rat cortical neurons are cultured and treated with sodium nitroprusside to induce mitochondrial dysfunction and apoptosis in the presence of various concentrations of edonerpic. Neuronal survival is assessed by MTT or LDH release assays.
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| Cell Assay |
Cellular assays for edonerpic use primary rat cortical neurons. Cells are treated with various concentrations of edonerpic. Mitochondrial dysfunction is induced by sodium nitroprusside. Mitochondrial membrane potential is assessed using fluorescent dyes (e.g., JC-1). Apoptosis is assessed by caspase-3/7 activity or Annexin V staining. These assays confirm the compound's neuroprotective activity.
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| Animal Protocol |
In vivo animal studies for edonerpic utilize models of neurodegenerative diseases, such as Alzheimer's disease models. The compound is administered orally or intraperitoneally at 8.4 mg/kg per day. Cognitive function is assessed using behavioral tests (e.g., Morris water maze). Amyloid-β levels and neuroinflammation are measured in brain tissue. Efficacy is compared to vehicle controls.
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| ADME/Pharmacokinetics |
Edonerpic maleate has molecular weight of 407.48 g/mol and molecular formula C20H25NO6S. It is a maleate salt. Purity is ≥98%. It is soluble in DMSO. It is typically stored at -20°C. Pharmacokinetic properties such as oral bioavailability and brain penetration would be determined in preclinical studies.
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| Toxicity/Toxicokinetics |
Preclinical toxicity of edonerpic has been evaluated in standard toxicology studies. As a neurotrophic agent, potential adverse effects may include CNS effects. No significant toxicity has been reported at therapeutic doses. The compound is for research use only and is not approved for clinical use.
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| References |
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| Additional Infomation |
Edonerpic maleate (T-817 maleate) is a novel neurotrophic agent. It inhibits amyloid-β peptides (Aβ). It protects against mitochondrial dysfunction and apoptosis in neurons. It has potential for neurodegenerative disease research. It is available for research purposes only.
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| Molecular Formula |
C20H25NO6S
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|---|---|
| Molecular Weight |
407.481
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| Exact Mass |
407.14
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| CAS # |
519187-97-4
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| Related CAS # |
519187-23-6;519187-97-4;
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| PubChem CID |
11338749
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
28
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| Complexity |
415
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1C(CN1CCCOCCC2=CC3=C(C=C2)SC=C3)O.C(=C\C(=O)O)\C(=O)O
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| InChi Key |
1-(3-(2-(benzo[b]thiophen-5-yl)ethoxy)propyl)azetidin-3-ol maleate
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| InChi Code |
RLUCYBFCLXANSO-BTJKTKAUSA-N
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| Chemical Name |
T-817 maleate T-817 T 817 T817 J2.179.155E T-817MA Edonerpic Edonerpic maleate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~245.41 mM)
H2O : ~100 mg/mL (~245.41 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.14 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.14 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 140 mg/mL (343.58 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4541 mL | 12.2705 mL | 24.5411 mL | |
| 5 mM | 0.4908 mL | 2.4541 mL | 4.9082 mL | |
| 10 mM | 0.2454 mL | 1.2271 mL | 2.4541 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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