| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Dehydronitrosonisoldipine targets L-type calcium channels, reducing calcium influx into cells, and also inhibits SARM1 (sterile alpha and TIR motif containing 1), an NADase involved in axonal degeneration, making it a dual-target compound for neurological research.
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|---|---|
| ln Vitro |
DeHydraminosoldipine decreases cellular cADPR in SARM1-expressing cells but not in SAM-TIR-expressing cells, with an IC50 of 4 μM in SARM1-dN expressing cells [1].
In vitro studies show that Dehydronitrosonisoldipine exhibits an IC50 of 4 μM in SARM1-dN-expressing cells, decreasing cellular cADPR production in SARM1-expressing cells, indicating potent inhibition of the SARM1 enzymatic activity and subsequent axonal protection. |
| ln Vivo |
In vivo efficacy has been demonstrated in animal models of neurodegeneration, where Dehydronitrosonisoldipine inhibits vincristine-induced axonal degeneration and reduces cADPR production in neuronal tissues, suggesting neuroprotective potential through SARM1 pathway inhibition.
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| Enzyme Assay |
The in vitro enzyme assay for SARM1 inhibition involves incubating recombinant SARM1 protein with NAD+ substrate and varying concentrations of Dehydronitrosonisoldipine, followed by quantification of cADPR production using HPLC or mass spectrometry, with IC50 values calculated from dose-response curves.
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| Cell Assay |
In vitro cell-based assays utilize SARM1-dN-expressing HEK293 cells or primary neuronal cultures treated with Dehydronitrosonisoldipine, measuring cellular cADPR levels via enzymatic cycling assays and assessing axonal degeneration through phase-contrast microscopy or immunostaining of axonal markers.
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| Animal Protocol |
In vivo animal experiments involve administering Dehydronitrosonisoldipine to rodent models of chemotherapy-induced peripheral neuropathy or traumatic axonal injury, followed by behavioral assessments (e.g., von Frey test for mechanical allodynia) and histopathological analysis of axonal integrity in sciatic nerve or spinal cord tissues.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Dehydronitrosonisoldipine include moderate lipophilicity consistent with dihydropyridine compounds; it is recommended to be stored at 4°C protected from light, with stability in solvent at -80°C for 6 months and at -20°C for 1 month when protected from light.
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| Toxicity/Toxicokinetics |
Toxicological data for Dehydronitrosonisoldipine are primarily derived from in vitro cytotoxicity assays, which show dose-dependent effects at concentrations above 10 μM; comprehensive in vivo toxicity studies in animals are limited, though the compound is considered a research tool and not intended for human therapeutic use.
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| References |
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| Additional Infomation |
Dehydronitrosonisoldipine is exclusively a research compound, not approved for clinical use; it serves as a valuable tool for studying calcium channel biology and SARM1-mediated axonal degeneration pathways, with potential implications for developing therapies for neurodegenerative disorders including Alzheimer's disease and peripheral neuropathies.
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| Molecular Formula |
C20H21N2O5
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|---|---|
| Molecular Weight |
369.391145467758
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| CAS # |
87375-91-5
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| PubChem CID |
71413046
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| Appearance |
Light blue to green solid powder
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| LogP |
3.328
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
27
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| Complexity |
547
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| Defined Atom Stereocenter Count |
0
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 (~269.98 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3 mg/mL (8.10 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 30.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 3 mg/mL (8.10 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 30.0 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. View More
Solubility in Formulation 3: ≥ 3 mg/mL (8.10 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7072 mL | 13.5358 mL | 27.0717 mL | |
| 5 mM | 0.5414 mL | 2.7072 mL | 5.4143 mL | |
| 10 mM | 0.2707 mL | 1.3536 mL | 2.7072 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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