| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
VP3.15 targets phosphodiesterase 7 (PDE7) and glycogen synthase kinase 3 (GSK-3). PDE7 is an enzyme that hydrolyzes cAMP, while GSK-3 is a multifunctional kinase involved in various signaling pathways. By inhibiting both targets, VP3.15 modulates neuroinflammation, synaptic plasticity, and neurodegenerative disease mechanisms.
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| ln Vitro |
In vitro, VP3.15 is a potent dual PDE7/GSK-3 inhibitor with IC50 values of 1.59 μM for PDE7 and 0.88 μM for GSK-3. Its activity is assessed using enzyme inhibition assays measuring PDE7-mediated cAMP hydrolysis and GSK-3-mediated substrate phosphorylation.
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| ln Vivo |
In vivo activity data for VP3.15 are limited in the available literature. As a CNS-penetrant compound with neuroprotective and neurorepair activities, it has potential applications in multiple sclerosis (MS) and other neurodegenerative disorders. Further in vivo studies are needed to evaluate its efficacy and safety.
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| Enzyme Assay |
In vitro enzyme inhibition assays for VP3.15 are performed using purified PDE7 and GSK-3 enzymes. For PDE7, enzyme activity is measured by quantifying cAMP hydrolysis using radiometric or fluorescent methods. For GSK-3, activity is measured by quantifying substrate phosphorylation using ELISA or radiometric methods. IC50 values (1.59 μM for PDE7, 0.88 μM for GSK-3) are calculated from inhibition curves.
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| Cell Assay |
In vitro cellular assays for VP3.15 are performed using neuronal cell lines or primary neurons. Cells are treated with the compound, and PDE7 and GSK-3 activities are assessed by measuring cAMP levels and substrate phosphorylation, respectively. Neuroprotective effects are evaluated by measuring cell viability following exposure to neurotoxic stimuli.
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| Animal Protocol |
In vivo animal experiments for VP3.15 are not extensively documented. As a potential therapeutic for neurodegenerative disorders, in vivo studies would typically involve administration to animal models of multiple sclerosis or other CNS diseases. The compound would be administered via oral or intraperitoneal routes, and efficacy would be assessed by measuring neuroinflammation, demyelination, and functional outcomes.
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| ADME/Pharmacokinetics |
VP3.15 Dihydrobromide has a molecular weight of 528.30 and molecular formula C₂₀H₂₄Br₂N₄OS. It has a purity of 98.22%. It is a CNS-penetrant compound. Further PK details are available from the manufacturer's data sheets.
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| Toxicity/Toxicokinetics |
Toxicological data for VP3.15 Dihydrobromide are not extensively reported. As a research-use compound, its safety profile has not been formally evaluated in comprehensive preclinical toxicology studies. The compound is intended for research purposes only and is not approved for human therapeutic use. Standard laboratory safety precautions should be followed when handling this compound.
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| References | |
| Additional Infomation |
VP3.15 Dihydrobromide is a potent, orally bioavailable, and CNS-penetrant dual inhibitor of PDE7 and GSK-3 with IC50 values of 1.59 μM and 0.88 μM, respectively. It has neuroprotective and neurorepair activities. This product is for research use only.
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| Molecular Formula |
C20H24BR2N4OS
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|---|---|
| Molecular Weight |
528.303761482239
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| Exact Mass |
528.001
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| CAS # |
1281681-33-1
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| Related CAS # |
VP3.15;1281681-54-6
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| PubChem CID |
57326492
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| Appearance |
Light yellow to yellow solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
28
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| Complexity |
506
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Br.Br.S1/C(/N=C(C2C=CC=CC=2)N1C1C=CC=CC=1)=N/CCN1CCOCC1
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| InChi Key |
CAJZOXQDSKOPBU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H22N4OS.2BrH/c1-3-7-17(8-4-1)19-22-20(21-11-12-23-13-15-25-16-14-23)26-24(19)18-9-5-2-6-10-18;;/h1-10H,11-16H2;2*1H
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| Chemical Name |
N-(2-morpholin-4-ylethyl)-2,3-diphenyl-1,2,4-thiadiazol-5-imine;dihydrobromide
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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 : ~62.5 mg/mL (~118.30 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.94 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 20.8 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: ≥ 2.08 mg/mL (3.94 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 20.8 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: ≥ 2.08 mg/mL (3.94 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 | 1.8929 mL | 9.4643 mL | 18.9286 mL | |
| 5 mM | 0.3786 mL | 1.8929 mL | 3.7857 mL | |
| 10 mM | 0.1893 mL | 0.9464 mL | 1.8929 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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