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| Targets |
beta-Amyloid 1-16 targets the same molecular pathways as the full-length amyloid-beta peptide, primarily involving metal ion binding and aggregation. The Abeta 1-16 fragment contains the metal-binding domain of the full-length Abeta peptide, which includes histidine residues that coordinate copper, zinc, and iron ions. This metal-binding activity is believed to play a role in the neurotoxicity of Abeta and the pathogenesis of Alzheimer's disease. The peptide fragment is also used as an antigen to study the immune response to Abeta and to generate antibodies for research and diagnostic applications. beta-Amyloid 1-16 does not have a traditional pharmacological target but is instead used as a research tool to study the biochemistry and pathology of Alzheimer's disease. Its interactions with metal ions and antibodies are the primary focus of research using this peptide.
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| ln Vitro |
In vitro, beta-Amyloid 1-16 is used to study the metal-binding properties of the amyloid-beta peptide. The fragment contains the metal-binding domain of full-length Abeta and is capable of coordinating copper, zinc, and iron ions. Studies using Abeta 1-16 have characterized the stoichiometry and affinity of metal binding to the Abeta peptide. The peptide fragment is also used to study the structure and conformation of the Abeta peptide, as the 1-16 region is one of the most well-characterized regions of the full-length peptide. In immunological assays, Abeta 1-16 is used as an antigen to detect antibodies against Abeta in patient samples or to generate monoclonal antibodies for research purposes. The peptide's activity in these assays is determined by its ability to bind metal ions or antibodies, rather than by traditional pharmacological activity measurements.
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| ln Vivo |
Examining the contribution of important histidine residues (His, His in mouse and His, His, His in human segments) to the Ab-Cu2+ interaction Model is thought to be possible with the β-amyloid(1-16) fragment. β-amyloid (1-16) targets histidine residues that bind to metal ions for oxidation. In Alzheimer's disease senile plaques, copper attaches to Aβ, and β-amyloid (1-16) takes part in the coordination of Cu2+ ions. Cu2+ and Zn2+ have been linked to damage from free radicals and amyloid neurotoxicity [1]. The smallest sequence of amino acids exhibiting a Cu coordination pattern including three histidines (His6, His13, and His14) is β-Amyloid(1-16). It is believed that β-Amyloid (1-16) has a role in metal binding [2]. Zinc ions interact with human beta-amyloid via its metal-binding domains 1–16. The two polypeptide chains of the rat Aβ(1-16) dimer have opposing C-tail orientations, which prevents the rat Aβ dimer from assembling into oligomer aggregates. Consequently, drug resistance could be caused by variations in the structure of the zinc-binding site between human and rat β-amyloid (1-16), their capacity to form regular cross-monomer connections, and the orientation of their hydrophobic C-tails. Rats are at risk for Alzheimer's disease [3].
In vivo, beta-Amyloid 1-16 is not typically administered as a therapeutic agent but is used in research contexts to study the immune response to Abeta or to generate antibodies. The peptide fragment is sometimes used as an immunogen to generate antibodies against Abeta in animal models. However, comprehensive in vivo efficacy studies using Abeta 1-16 as a therapeutic agent have not been reported, as the peptide is primarily a research tool rather than a drug candidate. The full-length Abeta peptide and its fragments are the subject of extensive research in the context of Alzheimer's disease, but Abeta 1-16 itself is not used as a therapeutic. The peptide's in vivo behavior is influenced by its rapid clearance and metabolism, characteristic of small peptides. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays are not directly applicable to beta-Amyloid 1-16, as the peptide is not an enzyme inhibitor or receptor ligand in the traditional sense. However, the peptide's metal-binding properties can be characterized using biochemical methods. Isothermal titration calorimetry (ITC) or surface plasmon resonance (SPR) can be used to measure the binding affinity of Abeta 1-16 to metal ions such as copper, zinc, and iron. Circular dichroism (CD) spectroscopy and nuclear magnetic resonance (NMR) spectroscopy are used to study the structure and conformation of the peptide. The peptide's ability to bind antibodies can be characterized using enzyme-linked immunosorbent assays (ELISA) or other immunoassays. Thioflavin T (ThT) fluorescence assays can be used to study the aggregation properties of the peptide, although Abeta 1-16 aggregates less readily than the full-length peptide. Each assay is performed under appropriate buffer conditions and with appropriate controls.
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| Cell Assay |
In vitro cellular assays for beta-Amyloid 1-16 are not standard, as the peptide is not a traditional pharmacological agent. However, the peptide can be used in cell-based studies to investigate the role of metal binding in Abeta toxicity. Neuronal cell lines such as SH-SY5Y or primary neurons can be treated with Abeta 1-16 in the presence or absence of metal ions to study metal-dependent toxicity. Cell viability is assessed using standard assays such as MTT or LDH release. The peptide's ability to bind to cell surface receptors or to be internalized by cells can be studied using fluorescently labeled peptide and flow cytometry or fluorescence microscopy. Immunological assays using Abeta 1-16 can be performed in cell-based systems to study antibody-antigen interactions. Cytotoxicity of the peptide is assessed in parallel to determine safe concentrations for experiments.
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| Animal Protocol |
In vivo animal studies for beta-Amyloid 1-16 are typically conducted in the context of immunization studies. Animals (usually mice or rabbits) are immunized with Abeta 1-16 conjugated to a carrier protein such as keyhole limpet hemocyanin (KLH) to generate antibodies against the Abeta peptide. Serum is collected and antibody titers are measured by ELISA. In some studies, Abeta 1-16 is used in passive immunization experiments where antibodies generated against the peptide are administered to animal models of Alzheimer's disease to study their effects on Abeta pathology. The peptide is not typically administered as a therapeutic agent in animal models. Animals are monitored for clinical signs and immune responses. Comprehensive efficacy studies using Abeta 1-16 as a therapeutic have not been reported.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of beta-Amyloid 1-16 are characteristic of a small peptide. The peptide has a molecular weight of 1955.01 g/mol and a molecular formula of C84H119N27O28. As a peptide, Abeta 1-16 is susceptible to proteolytic degradation and has a short half-life in circulation. The peptide is soluble in water and DMSO. Comprehensive pharmacokinetic parameters including half-life, volume of distribution, clearance, and bioavailability have not been extensively characterized for Abeta 1-16, as it is primarily a research tool rather than a therapeutic candidate. The peptide's stability in solution and under various storage conditions has been characterized. Further pharmacokinetic studies would be needed if the peptide were to be developed as a therapeutic.
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| Toxicity/Toxicokinetics |
beta-Amyloid 1-16 is intended for laboratory research use only and has not undergone comprehensive toxicology testing. As a fragment of the amyloid-beta peptide, Abeta 1-16 is less toxic than the full-length Abeta peptide, which is known to be neurotoxic. However, the peptide can still exhibit cytotoxicity at high concentrations or in the presence of metal ions. Standard in vitro cytotoxicity assays in neuronal cell lines are typically performed to assess the peptide's toxicity. In vivo, animals immunized with Abeta 1-16 are monitored for signs of toxicity including immune responses and clinical observations. Comprehensive toxicological characterization including genotoxicity and repeated-dose toxicity studies has not been reported for Abeta 1-16. The peptide is not approved for human use and is strictly intended for research purposes.
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| References |
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| Additional Infomation |
beta-Amyloid 1-16 (Amyloid beta-Protein (1-16)) is a synthetic peptide fragment corresponding to the first 16 amino acids of the amyloid-beta peptide. It is involved in metal binding and is used as a research tool to study the structure, aggregation, and metal-binding properties of the full-length Abeta peptide. The peptide has a molecular weight of 1955.01 g/mol and a molecular formula of C84H119N27O28. Abeta 1-16 is also used as an antigen to generate antibodies against Abeta for research and diagnostic applications. The peptide is not a therapeutic agent and has not entered clinical trials. It is available from research chemical suppliers for non-clinical research purposes only. beta-Amyloid 1-16 is a valuable research tool for studying the biochemistry and pathology of Alzheimer's disease, particularly the role of metal binding in Abeta neurotoxicity.
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| Molecular Formula |
C84H119N27O28
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| Molecular Weight |
1955.01
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| Exact Mass |
1953.871
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| CAS # |
131580-10-4
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| PubChem CID |
146156923
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| Appearance |
White to off-white solid powder
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| Density |
1.6±0.1 g/cm3
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| Index of Refraction |
1.696
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| LogP |
-6.41
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| Hydrogen Bond Donor Count |
31
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| Hydrogen Bond Acceptor Count |
34
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| Rotatable Bond Count |
65
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| Heavy Atom Count |
139
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| Complexity |
4200
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(C)C(C(=O)NC(CC1=CNC=N1)C(=O)NC(CC2=CNC=N2)C(=O)NC(CCC(=O)N)C(=O)NC(CCCCN)C(=O)O)NC(=O)C(CCC(=O)O)NC(=O)C(CC3=CC=C(C=C3)O)NC(=O)CNC(=O)C(CO)NC(=O)C(CC(=O)O)NC(=O)C(CC4=CNC=N4)NC(=O)C(CCCNC(=N)N)NC(=O)C(CC5=CC=CC=C5)NC(=O)C(CCC(=O)O)NC(=O)C(C)NC(=O)C(CC(=O)O)N
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| InChi Key |
PKSRFXGDLPWBBS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C84H119N27O28/c1-41(2)68(82(137)109-59(30-47-35-92-40-97-47)80(135)107-57(28-45-33-90-38-95-45)78(133)102-51(18-21-62(87)114)73(128)104-54(83(138)139)12-7-8-24-85)111-75(130)53(20-23-65(118)119)103-76(131)55(27-44-14-16-48(113)17-15-44)99-63(115)36-94-71(126)61(37-112)110-81(136)60(32-67(122)123)108-79(134)58(29-46-34-91-39-96-46)106-72(127)50(13-9-25-93-84(88)89)101-77(132)56(26-43-10-5-4-6-11-43)105-74(129)52(19-22-64(116)117)100-69(124)42(3)98-70(125)49(86)31-66(120)121/h4-6,10-11,14-17,33-35,38-42,49-61,68,112-113H,7-9,12-13,18-32,36-37,85-86H2,1-3H3,(H2,87,114)(H,90,95)(H,91,96)(H,92,97)(H,94,126)(H,98,125)(H,99,115)(H,100,124)(H,101,132)(H,102,133)(H,103,131)(H,104,128)(H,105,129)(H,106,127)(H,107,135)(H,108,134)(H,109,137)(H,110,136)(H,111,130)(H,116,117)(H,118,119)(H,120,121)(H,122,123)(H,138,139)(H4,88,89,93)
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| Chemical Name |
6-amino-2-[[5-amino-2-[[2-[[2-[[2-[[2-[[2-[[2-[[2-[[2-[[2-[[2-[[2-[[2-[2-[(2-amino-3-carboxypropanoyl)amino]propanoylamino]-4-carboxybutanoyl]amino]-3-phenylpropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-3-carboxypropanoyl]amino]-3-hydroxypropanoyl]amino]acetyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-4-carboxybutanoyl]amino]-3-methylbutanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-5-oxopentanoyl]amino]hexanoic acid
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.5115 mL | 2.5575 mL | 5.1151 mL | |
| 5 mM | 0.1023 mL | 0.5115 mL | 1.0230 mL | |
| 10 mM | 0.0512 mL | 0.2558 mL | 0.5115 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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