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| Targets |
beta-Amyloid (1-42) targets various neuronal surface receptors that mediate its neurotoxic effects. Abeta42 oligomers bind to several receptors, including the cellular prion protein (PrPc), metabotropic glutamate receptor 5 (mGluR5), NMDA receptors, Ephrin receptors, and the receptor for advanced glycation end products (RAGE). The monomeric form of Abeta1-42 exhibits antioxidant and neuroprotective properties, while the oligomeric and fibrillar forms are neurotoxic and contribute to synaptic dysfunction and neuronal death in Alzheimer‘s disease.
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| ln Vitro |
Guide to amyloid-β aggregation (The following is our recommended protocol. This protocol provides guidelines only and should be modified to suit your specific needs). 1. Dissolve solid Aβ peptide in cold hexafluoro-2-propanol (HFIP). Incubate the peptide at room temperature for at least 1 hour to establish monomerization and structural randomization. 2. Remove HFIP by evaporation and store the resulting peptide as a thin film at -20 or -80°C. 3. Dissolve the resulting film in 5mM anhydrous DMSO and then vortex to dilute to the appropriate concentration and buffer (media without serum and phenol red). 4. Next, incubate the solution at 4-8°C for 48 hours. The sample is then centrifuged at 14,000g for 10 minutes at 4-8°C; soluble oligomers are in the supernatant. Dilute the supernatant 10-200 times for experiments. Methods vary depending on downstream applications. Note: Aggregated forms are unstable in solution and are recommended for immediate use.
In vitro, beta-Amyloid (1-42), human TFA is the key peptide used to study Alzheimer‘s disease pathogenesis. Monomeric Abeta1-42 (freshly dissolved in appropriate solvents) exhibits antioxidant and neuroprotective effects. However, when allowed to aggregate, Abeta1-42 forms neurotoxic oligomers and fibrils that are the primary focus of AD research. These aggregated species bind to various neuronal surface receptors (PrPc, mGluR5, NMDA receptors, etc.), leading to neuronal dysfunction and death. The peptide is used to screen for anti-amyloid compounds that inhibit aggregation or disaggregate pre-formed fibrils. |
| ln Vivo |
β-Amyloid (1-42), human TFA can be used in animal modeling to construct Alzheimer's disease models.
beta-Amyloid (1-42), human TFA induces neurotoxicity and synaptic dysfunction in vivo. When injected into the brains of rodents, aggregated Abeta1-42 oligomers/fibrils cause memory deficits, neuronal loss, synaptic impairment, and neuroinflammation, modeling key aspects of Alzheimer‘s disease pathology. It is widely used to create acute or sub-acute AD models in mice and rats. The TFA salt form has been the industry standard for peptide production and is used in such in vivo studies. No specific dosing or efficacy data are provided in the search results. |
| Enzyme Assay |
The binding of Abeta1-42 oligomers to neuronal receptors is typically measured by surface plasmon resonance (SPR) or ELISA using purified recombinant receptors (e.g., PrPc, mGluR5). Abeta oligomers are prepared by incubating monomeric Abeta1-42 (1 mg/mL in HFIP, then dried and redissolved in DMSO, then diluted in PBS) at 4degC for 24-48 hours. The Abeta oligomers are immobilized on a sensor chip or plate, and the receptor proteins are flowed over them, or vice versa. Binding affinities (KD) are calculated. Alternatively, receptor binding is measured in membrane preparations from cells expressing the receptors, using radiolabeled Abeta. Aggregation kinetics are monitored by Thioflavin T (ThT) fluorescence.
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| Cell Assay |
For in vitro neurotoxicity assays, primary cortical or hippocampal neurons (isolated from embryonic day 16-18 rat or mouse embryos) are seeded in 96-well plates and cultured for 7-14 days in vitro. Abeta1-42 oligomers (5-20 microM) are prepared by incubating monomeric Abeta (in HFIP/ DMSO) in PBS at 4degC for 24-48 hours or by using commercial pre-formed fibrils (PFFs). Mature neurons are treated with Abeta1-42 oligomers for 24-72 hours. Neuronal viability is assessed by MTT, LDH, or Calcein-AM staining. Synaptic toxicity is assessed by measuring the loss of synaptic proteins (PSD-95, synaptophysin) by Western blot. Neuronal apoptosis is assessed by cleaved caspase-3 immunostaining. ROS levels are measured by DCFH-DA fluorescence.
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| Animal Protocol |
For in vivo evaluation of neurotoxicity and cognitive impairment, male Sprague-Dawley rats or C57BL/6 mice (8-12 weeks old) are used. Abeta1-42 oligomers (5-10 microg per animal in 5 microL PBS) are aggregated as described above. The Abeta peptide is then injected intracerebroventricularly (ICV, via stereotaxic surgery) or bilaterally into the hippocampus or lateral ventricles. A surgical sham group receives vehicle (PBS) injection. After 7-28 days post-injection, cognitive function is assessed using the Morris water maze (spatial memory), Y-maze (working memory), and passive avoidance test. At the study endpoint, brains are collected for histological analysis (Abeta immunohistochemistry, Thioflavin S staining for plaques), Western blot for synaptic markers and neuroinflammatory markers (Iba1 for microglia, GFAP for astrocytes), and ELISA for cytokines (IL-1beta, TNF-alpha, IL-6).
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| ADME/Pharmacokinetics |
beta-Amyloid (1-42), human TFA (C203H311N₅₅O₆0S·TFA, MW = 4514.1 for the peptide, plus TFA counterion) is a white to off-white lyophilized powder. For storage, the lyophilized powder should be kept at -20degC or -80degC, sealed, and protected from light and moisture. For in vitro use, the peptide is typically dissolved in hexafluoroisopropanol (HFIP) to monomerize, then dried, and redissolved in DMSO or PBS. Avoid repeated freeze-thaw cycles. The TFA salt is the industry standard for synthetic Abeta peptides. For cell culture, the TFA salt can be exchanged to HCl or acetate by repeated lyophilization from dilute HCl if needed. No PK data are applicable as the peptide is used for in vitro and ex vivo studies.
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| Toxicity/Toxicokinetics |
beta-Amyloid (1-42) is itself the toxic species being studied; its aggregated forms are neurotoxic. Monomeric Abeta1-42 has been reported to have antioxidant and neuroprotective effects, while oligomers and fibrils are neurotoxic. The TFA counterion may have its own toxicity at high concentrations but is present at low levels in typical assays. As a research compound, it is not intended for human or veterinary use. Standard laboratory safety precautions for handling neurotoxic peptides should be followed, including the use of gloves, lab coat, and safety goggles. Appropriate disposal procedures for hazardous biological materials should be followed.
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| References |
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| Additional Infomation |
beta-Amyloid (1-42), human TFA is the most widely used synthetic peptide for Alzheimer‘s disease research. Abeta1-42 is the longer and more aggregation-prone isoform of Abeta (the other major isoform is Abeta1-40). Abeta1-42 is the primary component of amyloid plaques in Alzheimer's disease and is believed to be the initiating factor in AD pathogenesis (the amyloid cascade hypothesis). The peptide is used to study the mechanism of Abeta aggregation, to screen for inhibitors of Abeta aggregation and toxicity, to develop antibodies and imaging probes for Abeta, and to create acute animal models of AD by direct injection into the brain. The TFA (trifluoroacetate) counterion improves the solubility and handling of the highly hydrophobic peptide. It should be noted that the monomeric form of Abeta1-42 is not toxic; the toxicity arises from the formation of soluble oligomers and protofibrils. The peptide is for research use only and has no therapeutic applications. It has not received regulatory approval for any indication. The CAS number for the TFA salt is often 107761-42-2 (or similar, depending on the supplier). The non-TFA (acetate or HCl) forms are also available. beta-Amyloid (1-42) is also known as Abeta42, Abeta42, or amyloid beta-peptide (1-42). The peptide sequence is: DAEFRHDSGYEVHHQKLVFFAEDVGSNKGAIIGLMVGGVVIA.
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| Molecular Formula |
C205H312F3N55O62S
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| Molecular Weight |
4628.06
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| Appearance |
Solid powder
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| Synonyms |
Amyloid β-peptide (1-42) (human) TFA
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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: (1). This product is not stable in solution, please use freshly prepared working solution for optimal results. (2). 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 : 33.33 mg/mL (7.20 mM; with sonication)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (0.54 mM)(Saturation unknown) in 10% DMSO 40% PEG300 5% Tween-80 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, add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix well; then add 50 μL Tween-80 to the above system and mix well; then add 450 μL saline to make up 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: 2.5 mg/mL (0.54 mM) in 10% DMSO 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension; sonication. For example, if 1 mL of working solution, add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD in saline and mix well. *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. Solubility in Formulation 3: ≥ 2.5 mg/mL (0.54 mM)(Saturation unknown) in 10% DMSO 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution, add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.2161 mL | 1.0804 mL | 2.1607 mL | |
| 5 mM | 0.0432 mL | 0.2161 mL | 0.4321 mL | |
| 10 mM | 0.0216 mL | 0.1080 mL | 0.2161 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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