VP3.15 dihydrobromide

Name: VP3.15 dihydrobromide
Brand: MedChemExpress
SKU: HY-128879A
Rating: 5.0 (3 reviews)

Cat. No.: HY-128879A Purity: 98.0%: Data Sheet
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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.

For research use only. We do not sell to patients.

VP3.15 dihydrobromide Chemical Structure

CAS No. : 1281681-33-1

Size	Stock	Quantity
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of VP3.15 dihydrobromide:

VP3.15 Get quote

3 Publications Citing Use of MCE VP3.15 dihydrobromide

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Phosphodiesterase (PDE) Isoform Specific Products:

View All Isoforms

PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

View All GSK-3 Isoform Specific Products:

View All Isoforms

GSK-3 GSK-3α GSK-3β

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

PDE7

In Vitro

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.

Immunofluorescence^[1]

Cell Line:	OPCs
Concentration:	1 μM
Incubation Time:	5, 7, 10 DIV
Result:	Significantly increased the number of mature oligodendrocytes (identified as double-positive cells of CNPase⁺-Olig2⁺ and MBP⁺-Olig2⁺).

Parmacokinetics

Species	Dose	Route	T_max (Plasma)	C_max	AUC_last	AUC_{INF_obs}	MRT_last	MRT_0-inf	T_max (Brain)	AUC_inf
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

In Vivo

VP3.15 dihydrobromide (10 mg/kg; i.p.; 3 alternate-day administrations (1-week group); 3 alternate-day administrations per week for a total of 3 doses (3-week group)/2-3 doses) significantly accelerates in vivo remyelination processes in Cuprizone (HY-W115718) and LPC demyelination models, and increases the myelin thickness of remyelinated fibers^[1].
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.

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]
Dosage:	10 mg/kg
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)
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.

Animal Model:	CD1 (7-day-old at study initiation)^[2]
Dosage:	10 mg/kg
Administration:	daily; 7 consecutive days (P7-P13)
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.

Molecular Weight

528.30

Formula

C₂₀H₂₄Br₂N₄OS

CAS No.

1281681-33-1

Appearance

Solid

Color

Light yellow to yellow

SMILES

[H]Br.[H]Br.N1(CC/N=C2N=C(C3=CC=CC=C3)N(C4=CC=CC=C4)S/2)CCOCC1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

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.
Protocol 2

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (3.94 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 98.0%

Select Batch:

Data Sheet (282 KB) SDS (252 KB)

COA (249 KB)

Handling Instructions (2659 KB)

References

[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.

Complete Stock Solution Preparation Table

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