VP3.15 dihydrobromide
Based on 3 publication(s) in Google Scholar
VP3.15 dihydrobromide is a highly potent, orally bioavailable, and CNS-penetrant PDE7-GSK3 dual inhibitor, with IC50 values of 1.59 μM and 0.88 μM against PDE7 and GSK3, respectively. VP3.15 dihydrobromide elevates intracellular cAMP levels, suppresses immune responses, enhances remyelination, limits excessive tau phosphorylation, and alleviates neuroinflammation and neuronal loss. VP3.15 dihydrobromide promotes oligodendrocyte precursor cell differentiation, improves in vivo remyelination, inhibits autoimmune encephalomyelitis, and mitigates germinal matrix-intraventricular hemorrhage-related brain injury, cerebral atrophy, ventricular enlargement, and cognitive impairment. VP3.15 dihydrobromide can be used in research related to multiple sclerosis and germinal matrix-intraventricular hemorrhage.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.0%
- CAS. Nr.: 1281681-33-1
- Formel: C20H24Br2N4OS
- Molecular Weight:528.30
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) VP3.15 dihydrobromide
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Biologische Aktivität
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PDE7 |
VP3.15 dihydrobromide exhibits an IC50 of 1.59 μM against PDE7 and an IC50 of 0.88 μM against GSK3 in cell-free biochemical assays[1].
VP3.15 dihydrobromide (1 μM; 5-10 DIV (in vitro culture days)) enhances the differentiation of oligodendrocyte precursor cells (OPCs) from P0 CD1 mice into CNPase+-Olig2+ and MBP+-Olig2+ mature oligodendrocytes, without altering the morphology of oligodendrocytes[1].
VP3.15 dihydrobromide (1 μM; 5 DIV) significantly promotes the differentiation of adult oligodendrocyte precursor cells (OPCs) into CNPase+ mature oligodendrocytes at 5 DIV without altering the morphology of oligodendrocytes[1].
VP3.15 dihydrobromide (5 μM; 1-3 DPL (days post-lesion)) significantly enhances remyelination at 3 DPL in demyelinated cerebellar slices from P7 CD1 mice induced by Lysophosphatidylcholines (LPC) (HY-139414), whereas no effect is observed at 1 DPL[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:OPCs
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Concentration:1 μM
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Incubation Time:5, 7, 10 DIV
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Result:Significantly increased the number of mature oligodendrocytes (identified as double-positive cells of CNPase+-Olig2+ and MBP+-Olig2+).
| Species | Dose | Route | Tmax (Plasma) | Cmax | AUClast | AUCINF_obs | MRTlast | MRT0-inf | Tmax (Brain) | AUCinf |
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| Mice[1] | 10 mg/kg | i.p. | 0.25 h | 1990.43 ng/mL | 1956.74 ng·h/mL | 1998.55 ng·h/mL | 0.82 h | 0.91 h | 0.08 h | 1506.00 h·ng/g |
| Mice[1] | 50 mg/kg | p.o. | 1.00 h | 880.76 ng/mL | 2292.94 ng·h/mL | / | 1.64 h | 1.86 h | 0.5 h | 2378.17 ng·h/mL |
VP3.15 dihydrobromide (10 mg/kg; daily for 7 consecutive days) improves cognitive impairment, reduces hemorrhage and microglial burden, limits brain atrophy, restores neuronal density and myelination, promotes neurogenesis, and normalizes p-GLS levels in mice with intraventricular hemorrhage[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57/BL6 (8-week-old male, demyelination induced by 5 weeks of ad libitum feeding with 0.2% Cuprizone mixed with milled chow/focal demyelination induced by stereotactic injection of 2 μl of 1% LPC into the corpus callosum)[1]
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Dosage:10 mg/kg
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Administration:i.p.; 3 alternate days (1-week group); 3 doses per week on alternate days (3-week group)/2 doses (14 dpi group); 3 doses (21 dpi group)
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Result:Showed significantly higher eriochrome cyanine myelin staining and MBP fluorescence intensity in the corpus callosum one week after cuprizone withdrawal.
Had a significantly lower number of PDGFRα+ oligodendrocyte progenitor cells (OPCs) in the corpus callosum one week after cuprizone withdrawal.
Exhibited equivalent myelin staining (eriochrome cyanine and MBP) and OPC counts compared to vehicle controls three weeks after cuprizone withdrawal.
Showed no changes in microglial activation or astrocyte immunoreactivity compared to vehicle controls.
Significantly increased myelin sheath thickness (reduced G-ratio) compared to vehicle controls at both 14 and 21 dpi, with values approaching those of unlesioned control mice without evidence of hypermyelination.
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Animal Model:CD1 (7-day-old at study initiation)[2]
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Dosage:10 mg/kg
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Administration:daily; 7 consecutive days (P7-P13)
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Result:Improved learning in the Morris Water Maze (MWM) acquisition phase, restored time spent and number of entries in the target quadrant during 24-hour and 72-hour MWM retention tests, and normalized performance in the "where" paradigm of the New Object Discrimination test, compared to untreated GM-IVH mice.
Significantly reduced hemorrhage burden in the cortex at P14 and completely reversed cortical hemorrhage burden to control levels at P110; reduced hemorrhage burden in the hippocampus and striatum at P14, with a non-significant trend toward reduction at P110.
Reduced Iba1+ microglial burden to control levels in the cortex, hippocampus, and subventricular zone (SVZ) at P14; limited microglial burden increases in these regions at P110 compared to untreated GM-IVH mice.
Ameliorated reductions in brain weight at P14 and P110; significantly improved hemisection size at P110, normalized cortical size reductions at P14 and P110, and reduced ventricle enlargement at both time points compared to untreated GM-IVH mice.
Restored NeuN/DAPI ratios (neuronal density) in the cortex and SVZ at P14, and in the hippocampus at P110; reduced tau hyperphosphorylation (p-tau/total tau ratio) in the cortex at P110 to match control levels; restored myelin basic protein (MBP) levels in the cortex at P14.
Increased BrdU+ cell counts (proliferation), DCX+ area (neurogenesis), and BrdU/DCX ratio in the SVZ at P14; restored BrdU+ cell counts, DCX+ cell counts, and BrdU/DCX ratio in the dentate gyrus (DG) at P110, and normalized DCX+ cell counts in the DG at P14 compared to untreated GM-IVH mice.
Restored plasma gelsolin (p-GLS) levels to control values at P110.
Chemical Information
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CAS. Nr. 1281681-33-1
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Appearance Solid
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Molecular Weight 528.30
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Formel C20H24Br2N4OS
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Color Light yellow to yellow
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SMILES
[H]Br.[H]Br.N1(CC/N=C2N=C(C3=CC=CC=C3)N(C4=CC=CC=C4)S/2)CCOCC1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (3)
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Journal Impact Factor
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Most Recent
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J Biol Chem
REDD1-dependent GSK3β signaling in podocytes promotes canonical NF-κB activation in diabetic nephropathy. [Abstract]2025 Mar;301(3):108244. PMID: 39880090 -
J Biol Chem
REDD1-dependent GSK3β dephosphorylation promotes NF-κB activation and macrophage infiltration in the retina of diabetic mice. [Abstract]2023 Aug;299(8):104991. PMID: 37392853 -
Lösungsmittel & Löslichkeit
DMSO : 62.5 mg/mL (118.30 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.94 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (3.94 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
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Data Sheet (282 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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Handling Instructions (2659 KB)
Verweise
[1]. Medina-Rodríguez EM, et al. Promoting in vivo remyelination with small molecules: a neuroreparative pharmacological treatment for Multiple Sclerosis. Sci Rep. 2017;7:43545. Published 2017 Mar 3. [Content Brief]
[2]. Atienza-Navarro I, et al. Glycogen Synthase Kinase-3β Inhibitor VP3.15 Ameliorates Neurogenesis, Neuronal Loss and Cognitive Impairment in a Model of Germinal Matrix-intraventricular Hemorrhage of the Preterm Newborn. Transl Stroke Res. 2025 Apr;16(2):467-483. [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 (sealed storage, away from moisture). 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 | 1.8929 mL | 9.4643 mL | 18.9286 mL | 47.3216 mL |
| 5 mM | 0.3786 mL | 1.8929 mL | 3.7857 mL | 9.4643 mL | |
| 10 mM | 0.1893 mL | 0.9464 mL | 1.8929 mL | 4.7322 mL | |
| 15 mM | 0.1262 mL | 0.6310 mL | 1.2619 mL | 3.1548 mL | |
| 20 mM | 0.0946 mL | 0.4732 mL | 0.9464 mL | 2.3661 mL | |
| 25 mM | 0.0757 mL | 0.3786 mL | 0.7571 mL | 1.8929 mL | |
| 30 mM | 0.0631 mL | 0.3155 mL | 0.6310 mL | 1.5774 mL | |
| 40 mM | 0.0473 mL | 0.2366 mL | 0.4732 mL | 1.1830 mL | |
| 50 mM | 0.0379 mL | 0.1893 mL | 0.3786 mL | 0.9464 mL | |
| 60 mM | 0.0315 mL | 0.1577 mL | 0.3155 mL | 0.7887 mL | |
| 80 mM | 0.0237 mL | 0.1183 mL | 0.2366 mL | 0.5915 mL | |
| 100 mM | 0.0189 mL | 0.0946 mL | 0.1893 mL | 0.4732 mL |
VP3.15 dihydrobromide Related Classifications
HY-128879A Related Classifications
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