Vasculotide
Based on 1 Customer Validation
Vasculotide is a blood-brain barrier (BBB)-penetrant Tie2 agonist. Vasculotide binds to a unique domain of Tie2, induces receptor clustering to drive phosphorylation, activates downstream PI3K/Akt and eNOS pathways, enhances inter-endothelial cell junctions (such as VE-cadherin and claudin-5), and inhibits inflammatory adhesion molecules, ultimately stabilizing the vascular endothelial barrier and reducing its permeability. Vasculotide alleviates pulmonary microvascular leakage and microcirculatory dysfunction caused by cardiopulmonary bypass, acts as an adjuvant radioprotective agent to reduce acute radiation dermatitis, and promotes BBB recovery after focused ultrasound (FUS). Combination of Vasculotide with antibiotics reduces lung injury.
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- Pureza: 99.84%
- No. CAS: 1359657-45-6
- Peso molecular:14000 (average)
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Almacenamiento:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Vasculotide (28 ng/mL; 3 h) enhances the clonogenic survival rate of irradiated HMVEChTERT cells, with a significant SER value of 1.17[2].
Vasculotide (28 ng/mL; 3 h) preserves the angiogenic capacity of HMVEChTERTs exposed to 4 Gy irradiation, resulting in the formation of tubules comparable to those of non-irradiated cells[2].
Vasculotide (15 min) stimulates the phosphorylation of Tie2 receptors in HMVEChTERTs and activates the downstream AKT pro-survival pathway[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Vasculotide (10 μg/kg; intraperitoneal injection; administered 24 h and 1.5 h prior to irradiation, followed by once every other day for 28 consecutive days) reduces acute cutaneous radiation injury in mice, as evidenced by a 43% reduction in the total area of severe desquamation wounds, alleviated inflammatory responses, and improved wound healing[2].
Vasculotide (10 μg/kg; i.p.; pre-irradiation only, continuous administration, post-irradiation only; total 26 days) reduces acute cutaneous radiation injury in mice exposed to 35 Gy irradiation when administered via all tested regimens (pre-irradiation, continuous administration, post-irradiation), among which the post-irradiation regimen significantly decreases the overall skin injury score by 28%[2].
Vasculotide (250 ng; intraperitoneal injection; once every 48 hours; for 3 months) reduces the superharmonic threshold pressure for focused ultrasound (FUS)-induced blood-brain barrier (BBB) permeability by 21-29% in TgCRND8 mice and accelerates BBB repair, with an 87% BBB closure rate observed 20 hours after FUS treatment in this Alzheimer's disease model[3].
Adjuvant therapy with Vasculotide (500 ng; intravenous injection; 2 administrations) combined with Ampicillin (HY-B0522) significantly reduces pulmonary permeability, ventilator-induced lung injury (VILI)-related histological damage and edema formation in mice with mechanically ventilated Streptococcus pneumoniae pneumonia, without affecting immune responses or bacterial loads[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar (male, 375-425 g)[1]
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Dosage:200 ng
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Administration:i.v.; single dose
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Result:Completely preserved microcirculatory perfusion during and after CPB, with the number of continuously perfused and non-perfused vessels remaining stable throughout the experiment.
Significantly reduced Evans blue dye extravasation in lung tissue compared with untreated CPB rats.
Did not significantly reduce leakage in kidney tissue.
Did not affect circulating concentrations of angiopoietin-1, angiopoietin-2, or soluble Tie2.
Did not affect angiopoietin-1, angiopoietin-2, or Tie2 gene/protein expression in kidney or lung tissue, or endothelial adhesion molecule expression compared with untreated CPB rats.
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Animal Model:athymic nude mice (7-week-old female)[2]
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Dosage:10 μg/kg
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Administration:i.p.; 24 h and 1.5 h before irradiation, then every other day; 28 days
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Result:Reduced skin damage scores on day 6 and day 8, with no significant difference in overall area under the curve.
Reduced mean severe desquamation wound area overall, with peak areas reduced on day 12 and day 14.
Reduced weight loss 2 days post-irradiation, with full weight recovery by day 28.
Lowered oxygenated hemoglobin (oxyHb) levels overall, with trends toward lower levels on day 5, day 9, and day 12.
Reduced myeloperoxidase bioluminescence signal 6.4-fold lower than PBS at 72 h post-irradiation, and reduced neutrophil counts in skin sections on day 5.
Reduced serum MIP-2/CXCL2 levels on day 5 post-irradiation.
Increased CD31+ microvascular endothelial cell staining-to-area ratio on day 14 post-irradiation, with no significant difference in CD45+ leukocyte staining.
Reduced ulcerated wounds by day 28 post-irradiation (1 of 5 vs. 4 of 5 in PBS group), with histological evidence of better healing.
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Animal Model:athymic nude mice (7-week-old female)[2]
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Dosage:10 μg/kg
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Administration:i.p.; pre-irradiation only (24 h and 1.5 h before irradiation); continuous (24 h and 1.5 h before irradiation, then every other day); post-irradiation only (starting 2 days after irradiation, then every other day); 26 days
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Result:Reduced overall skin damage scores with post-irradiation treatment, with higher body weight by day 26 and significantly reduced myeloperoxidase bioluminescence on day 23 post-irradiation.
Reduced total wound size overall with pre-irradiation, continuous, and post-irradiation treatments.
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Animal Model:Mixed C57/C3H background (male and female, 3 months old at study start; transgenic TgCRND8 with double amyloid precursor protein mutations KM670/671NL, V717F; non-transgenic littermate controls)[3]
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Dosage:250 ng
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Administration:i.p.; every 48 hours; 3 months
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Result:Reduced the ultra-harmonic threshold pressure for FUS-induced BBB permeability by 21-29% compared to all other groups.
Did not alter initial gadolinium enhancement post-FUS in either TgCRND8 or non-transgenic mice.
Accelerated BBB closure in TgCRND8 mice: at 6, 12, and 20 hours post-FUS, 26%, 17%, and 13% of focal spots remained permeable to gadolinium, respectively, leading to 87% BBB closure by 20 hours.
Resulted in 61%, 26%, and 26% of focal spots remaining permeable to gadolinium at 6, 12, and 20 hours post-FUS in non-transgenic mice, respectively, leading to 74% BBB closure by 20 hours.
Showed a statistically significant difference in BBB closure rate between Vasculotide-treated and PBS-treated TgCRND8 mice via log-rank analysis.
Led to no detectable Evans blue dye in the brain at 24 hours post-FUS in both Vasculotide-treated TgCRND8 and non-transgenic mice, indicating complete BBB impermeability.
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Animal Model:C57BL/6N (female, 8-10 weeks old, 18-20 g, intranasal inoculation with 5 × 106 CFU Streptococcus pneumoniae serotype 3 followed by 6 hours of mechanical ventilation starting 24 hours post-infection)[4]
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Dosage:500 ng (first dose); 500 ng (second dose)
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Administration:i.v.; 2 doses (22 hours post-infection, 1.5 hours prior to experiment termination)
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Result:Significantly reduced pulmonary hyperpermeability (measured as HSA BALF/plasma ratio) compared to ampicillin monotherapy.
Reduced the percentage of lung area affected by VILI compared to ampicillin monotherapy or untreated mice.
Reduced VILI severity scores compared to ampicillin monotherapy or untreated mice.
Diminished alveolar edema formation in VILI-affected lung areas compared to ampicillin monotherapy or untreated mice.
Reduced perivascular edema formation in pneumonia-affected lung areas compared to ampicillin monotherapy or untreated mice.
Did not alter pulmonary or systemic leukocyte counts, cytokine/chemokine production, local or systemic bacterial burden, pulmonary Tie2 mRNA expression, or pulmonary Tie2 phosphorylation.
Chemical Information
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No. CAS 1359657-45-6
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Appearance Solid
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Peso molecular 14000 (average)
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Color White to off-white
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvente y solubilidad
DMSO : 50 mg/mL (Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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: ≥ 2.5 mg/mL; Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL; Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Pureza y Documentación
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Ficha de datos (283 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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Dekker NAM, et al. Vasculotide, an angiopoietin-1 mimetic, reduces pulmonary vascular leakage and preserves microcirculatory perfusion during cardiopulmonary bypass in rats. Br J Anaesth. 2018;121(5):1041-1051. [Content Brief]
[2]. Korpela E, et al. Vasculotide, an Angiopoietin-1 mimetic, reduces acute skin ionizing radiation damage in a preclinical mouse model. BMC Cancer. 2014;14:614. Published 2014 Aug 26. [Content Brief]
[3]. Lynch M, et al. Vasculotide restores the blood-brain barrier after focused ultrasound-induced permeability in a mouse model of Alzheimer's disease. Int J Med Sci. 2021;18(2):482-493. Published 2021 Jan 1. [Content Brief]
[4]. Lask A, et al. Adjunctive therapy with the Tie2 agonist Vasculotide reduces pulmonary permeability in Streptococcus pneumoniae infected and mechanically ventilated mice. Sci Rep. 2022;12(1):15531. Published 2022 Sep 15. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Vasculotide Related Classifications
HY-P10580 Related Classifications
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