| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
Low-density lipoprotein receptor-related protein 1 (LRP1). This receptor is overexpressed on brain microvascular endothelial cells (BBB) and on various brain tumor cells, making Angiopep-2 an effective targeting ligand for CNS drug delivery.
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| ln Vitro |
The brain peptide carrier Angiopep-2 hydrochloride and paclitaxel combine to form ANG1005, a conjugation known as paclitaxel-Angiopep-2 hydrochloride. ANG1005 circumvents P-gp and penetrates the brain more than paclitaxel. Based on human cancer cell lines, ANG1005 exhibits anti-tumor effects akin to those of paclitaxel [1].
In 2D cell culture models using human cerebral microvascular endothelial cells (hCMEC/D3), Angiopep-2 density positively correlates with nanoparticle association. It shows high uptake in LRP1-overexpressing cell lines such as bEnd.3 and U87 cells, with the L-form displaying higher binding affinity than the D-form. |
| ln Vivo |
In mice implanted intracerebrally with NCI-H460 lung cancer cells or U87 MG glioblastoma cells, the administration of ANG1005 markedly increased the survival rate [1].
In mouse models, Angiopep-2-functionalized nanoparticles and conjugates show significantly enhanced brain accumulation, with in situ brain perfusion studies demonstrating up to 10-fold greater BBB transport efficiency compared to non-targeted controls. It improves drug penetration and retention in the brain. |
| Enzyme Assay |
Receptor binding assays use surface plasmon resonance (SPR) or radioligand competition binding with LRP1-overexpressing cell membranes. The interaction involves electrostatic interactions with LRP1 domains, and binding affinity can be measured by incubating labeled peptide with LRP1 and quantifying bound ligand after filtration.
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| Cell Assay |
In vitro BBB models consist of hCMEC/D3 cells cultured on Transwell inserts to form tight monolayers. Angiopep-2-conjugated nanoparticles or fluorescently labeled peptides are added to the apical chamber, and transport across the monolayer is measured by sampling the basolateral chamber and quantifying via fluorometry or mass spectrometry.
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| Animal Protocol |
In mouse xenograft models of glioblastoma (U87 MG tumors), animals are administered intravenous injections of Angiopep-2-conjugated drug-loaded nanoparticles or peptide-drug conjugates. Brain accumulation is measured by in vivo imaging, tissue dissection and analysis, or in situ brain perfusion. Tumor growth inhibition and survival are monitored.
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| ADME/Pharmacokinetics |
Angiopep-2 has a relatively short half-life due to rapid proteolytic degradation. Its in situ brain perfusion uptake (% input) is approximately 0.035 +/- 0.005, and conjugation to PEG or encapsulation in nanoparticles can significantly improve its pharmacokinetic profile and brain bioavailability.
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| Toxicity/Toxicokinetics |
In animal studies, Angiopep-2-functionalized delivery systems show no detectable tissue toxicity or abnormalities in H&E staining at therapeutic doses. No systemic toxicity or activation of innate immune response has been reported in standard efficacy studies.
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| References | |
| Additional Infomation |
Angiopep-2 is derived from aprotinin and shares sequence homology with the Kunitz domain. It is not approved for clinical use but is a widely studied research tool for BBB targeting. Phase 1 trials for ANG1005 (Angiopep-2-paclitaxel conjugate) have been completed for brain cancers.
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| Molecular Formula |
C104H150CLN29O31
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|---|---|
| Molecular Weight |
2337.93
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| Appearance |
White to off-white solid powder
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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) |
H2O :~100 mg/mL (~42.77 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (42.77 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.4277 mL | 2.1386 mL | 4.2773 mL | |
| 5 mM | 0.0855 mL | 0.4277 mL | 0.8555 mL | |
| 10 mM | 0.0428 mL | 0.2139 mL | 0.4277 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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