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Apelin-13, molecular formula C69H111N23O16S, CAS 217082-58-1. As an endogenous ligand for the G protein coupled receptor angiotensin II protein J (APJ), it is a peptide sequence consisting of 13 amino acids present in the central and peripheral nervous systems. Its unique structure and properties endow it with various important physiological and pathological functions in living organisms. Structurally, the peptide sequence of Apeli-13 enables it to tightly bind to APJ receptors, thereby activating G protein coupled receptors. The key indicator of this activation effect is the EC50 value, which is the concentration required to reach half of the maximum effect. The EC50 value of Apeli-13 is 0.37 nM, indicating its strong binding ability to APJ receptors.
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Customized Bottle Caps And Corks:
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Apelin-13 COA
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| Certificate of Analysis | ||
| Compound name | Apelin-13 | |
| Grade | Pharmaceutical grade | |
| CAS No. | 217082-58-1 | |
| Quantity | 37g | |
| Packaging standard | PE bag+Al foil bag | |
| Manufacturer | Shaanxi BLOOM TECH Co., Ltd | |
| Lot No. | 202512090051 | |
| MFG | Dec 9th 2025 | |
| EXP | Dec 8th 2028 | |
| Structure |
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| Item | Enterprise standard | Analysis result |
| Appearance | White or almost white powder | Conformed |
| Water content | ≤5.0% | 0.72% |
| Loss on drying | ≤1.0% | 0.33% |
| Heavy Metals | Pb≤0.5ppm | N.D. |
| As≤0.5ppm | N.D. | |
| Hg≤0.5ppm | N.D. | |
| Cd≤0.5ppm | N.D. | |
| Purity (HPLC) | ≥99.0% | 99.90% |
| Single impurity | <0.8% | 0.24% |
| Total microbial count | ≤750cfu/g | 95 |
| E. Coli | ≤2MPN/g | N.D. |
| Salmonella | N.D. | N.D. |
| Ethanol (by GC) | ≤5000ppm | 612ppm |
| Storage | Store in a sealed, dark, and dry place below -20°C | |
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Chemical Formula |
C69H111N23O16S |
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Exact Mass |
1550 |
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Molecular Weight |
1551 |
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m/z |
1550 (100.0%), 1551 (74.6%), 1552 (27.4%), 1551 (7.8%), 1553 (6.6%), 1552 (6.3%), 1552 (4.5%), 1553 (3.4%), 1552 (3.3%), 1553 (2.5%), 1553 (2.2%), 1551 (1.3%), 1554 (1.2%) |
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Elemental Analysis |
C, 53.44; H, 7.21; N, 20.77; O, 16.51; S, 2.07 |
In terms of physiological function, Apeli-13 mainly acts on the peripheral and central nervous systems, playing an important role in regulating cardiovascular function, fluid homeostasis, hypertension, and insulin sensitivity. Especially in terms of vasodilation and blood pressure reduction, Apeli-13 has shown significant effects. This makes it have potential application value in the treatment of cardiovascular diseases and hypertension.
Apelin-13 is a peptide hormone composed of 13 amino acids, mainly involved in regulating various physiological and pathological processes by binding to the G protein coupled receptor APJ.
1. Cardiovascular system:
-Vasodilatory effect: It can cause vasodilation by acting on vascular smooth muscle cells, thereby reducing vascular resistance, increasing blood flow, and lowering blood pressure.
-Cardioprotective effect: Studies have shown that it has a protective effect in the heart, can alleviate myocardial ischemia-reperfusion injury, prevent myocardial fibrosis, and may contribute to the recovery of heart function.
2. Metabolic regulation:
-Glucose metabolism: It may be involved in regulating glucose metabolism, and some studies have shown that it can promote insulin sensitivity and lower blood sugar levels.
-Lipid metabolism: It may also affect lipid metabolism, regulate the physiological function of adipose tissue, and have potential therapeutic value for obesity and related metabolic diseases.
3. Neurosystem:
-Neuroregulation: Its expression and function in the central nervous system have been extensively studied. It may be involved in neural functions such as appetite regulation, sleep regulation, and emotional regulation.
-Neuroprotection: Some studies suggest that Apelin-13 may have a protective effect on the nervous system, helping to prevent the occurrence and development of neurodegenerative diseases.
4. Immune regulation:
-Immune regulation: Studies have shown that Apelin-13 may participate in the body's immune regulation process through multiple pathways, including regulating the intensity of inflammatory responses and modulating the activity of key immune cells (such as macrophages and lymphocytes). By balancing immune and inflammatory responses, it has potential therapeutic effects on various inflammatory diseases, providing a new direction for the clinical treatment of such diseases.
5. Tumor Biology:
-Tumor occurrence and development: Some in vitro and in vivo studies have shown that Apelin-13 may play an important regulatory role in tumor biology. Its expression level in tumor tissues and peripheral blood is closely related to the occurrence, progression, and distant metastasis of various tumors. Due to this specific correlation, Apelin-13 may become a potential biomarker for tumor targeted treatment and prognosis evaluation, helping to improve the accuracy of tumor diagnosis and treatment effect evaluation.
6. Other functions:
-Reproductive regulation: may be involved in regulating the function of the reproductive system, affecting the secretion of reproductive hormones and the function of reproductive cells.
-Bone metabolism: Some studies suggest that it may have an impact on bone metabolism, participate in the proliferation and differentiation of bone cells, and have potential impacts on bone health.
7. Inflammatory regulation:
It may regulate the inflammatory response by affecting the release of inflammatory mediators and the activity of immune cells. This may have therapeutic potential for inflammatory diseases such as rheumatoid arthritis and inflammatory bowel disease.
8. Angiogenesis:
Some studies suggest that Apelin-13 may be closely involved in regulating the process of angiogenesis. It can promote the proliferation and directed migration of vascular endothelial cells, which are the core components of blood vessel formation, and further contribute to the regeneration and repair of damaged blood vessels, playing a positive role in vascular homeostasis and tissue repair.
9. Water electrolyte balance:
It may have potential diuretic and antihypertensive effects by affecting the water and electrolyte regulation function of the kidneys, affecting fluid balance and blood pressure regulation.
10. Drug development:
The APJ and its related receptors have become a research hotspot in drug development, and are expected to become targets for the treatment of cardiovascular diseases, metabolic diseases, neurological diseases, and more.
Apelin-13 is a peptide hormone, and its pharmacokinetic properties are crucial for understanding its absorption, distribution, metabolism, and excretion processes in vivo.
Usually administered by injection or oral administration. In the case of oral administration, it may be degraded by gastric acid and gastrointestinal enzymes, thereby affecting its absorption efficiency. Injection administration can bypass the gastrointestinal tract and directly enter the circulatory system, resulting in faster and more complete absorption.
The distribution characteristics within the body are not fully understood. Due to its small molecular weight and peptide structure, its distribution range may be limited by tissue and cell membranes, mainly concentrated in the circulatory system and some specific tissues.
The metabolic pathways and metabolites have not been fully elucidated. Due to its peptide like structure, it may be degraded and metabolized by proteases. The liver may be one of its main metabolic organs, but the specific metabolic pathways and metabolites require further research.
The excretory pathway is not yet fully understood. It may be excreted through pathways such as the kidneys and bile. There are no detailed research reports on its excretion kinetics yet.
-At present, there is limited understanding of its pharmacokinetic parameters, such as clearance rate, half-life, etc. These parameters are crucial for determining their drug concentration in vivo and maintaining appropriate treatment levels, and more experimental research is needed to determine them.
Pharmacokinetics is influenced by various factors, including individual differences, administration routes, doses, and possible interactions. These factors may affect their absorption, distribution, metabolism, and excretion processes in the body.
Molecular Structure and Composition
Amino acid sequence and modifications
Apelin-13 consists of 13 amino acids, with its core sequence being QRPRLSHKGPMPF (single-letter code), corresponding to the trinucleotide sequence Gln-Arg-Pro-Arg-Leu-Ser-His-Lys-Gly-Pro-Met-Pro-Phe.
C-terminal amidation: The C-terminal (Phe) of the natural Apelin-13 usually exists in an amide form (i.e., -NH₂), and this modification enhances its binding stability to the APJ receptor.
Derivative differences: Some derivatives (such as [Pyr1]-Apelin-13) are modified by N-terminal pyridine amidation (Pyr), significantly improving metabolic stability while retaining biological activity.
Molecular formula and molecular weight
Natural Apelin-13: The molecular formula is C₆₉H₁₁₁N₂₃O₁₆S, with a molecular weight of 1550.83 Da (free base form).
Trifluoroacetate (TFA) form: Due to the binding of the trifluoroacetic acid (TFA) molecule, the molecular weight increases to approximately 1651.94 Da (as C₇₉H₁₂₀N₂₀O₁₉, containing the TFA part).
[Pyr1]-Apelin-13: The molecular formula is C₆₉H₁₀₈N₂₂O₁₆S, with a molecular weight of 1533.8 Da, as the N-terminal modification reduces one hydrogen atom.
Secondary structure characteristics
α-Helix tendency: In solution, Apelin-13 may form local α-helical structures, especially in the hydrophobic regions (such as Trp, Phe, Leu, etc.), which are crucial for its binding to the APJ receptor.
Hydrophobic core: Hydrophobic amino acids such as tryptophan (Trp), phenylalanine (Phe), and leucine (Leu) form the core, stabilizing the peptide chain conformation and participating in receptor interaction.
Physical and Chemical Properties
Solubility and Stability
Solubility:
Natural Apelin-13 is soluble in PBS (pH 7.2) up to approximately 10 mg/mL, and has a higher solubility in DMSO (>155 mg/mL).
[Pyr1]-Apelin-13 has a solubility of 1 mg/mL in water, and its solubility needs to be optimized by adjusting the solvent (such as acetonitrile/water containing 0.1% TFA).
Stability:
Freeze-dried powder can be stably stored at -20℃ for at least 6 months. After reconstitution, it should be avoided from repeated freezing and thawing.
Stability under acidic conditions (such as pH 3.5-4.0) is relatively high, and it is prone to degradation in neutral or alkaline environments.
Acid-base properties
pI (equilibrium point): Not directly reported, but based on the amino acid composition, it is estimated to be close to neutral (pH 6.5-7.5).
pKa (acid dissociation constant): Predicted value is 3.56 ± 0.10, indicating that it carries a negative charge in physiological pH, which may affect its interaction with receptors or cell membranes.
Density and morphology
Density: Predicted value is 1.50 ± 0.1 g/cm³ (natural Apelin-13), and the derivatives may have slight differences due to modifications.
Morphology: Usually white or off-white freeze-dried powder, and after reconstitution, it is a transparent solution.
Chemical Stability and Degradation Pathways
Enzymatic sensitivity
Apelin-13 is easily degraded by serum's dipeptidyl peptidase-4 (DPP-4) and neutral endopeptidase (NEP), resulting in a short half-life (about several minutes).
[Pyr1]-Apelin-13 significantly resists DPP-4 degradation through N-terminal modification, prolonging its half-life in the body.
Oxidation and aggregation
Sulfur-containing amino acids (such as Met) are prone to oxidation, and need to be stored in the dark and added with antioxidants (such as 0.1% BSA). At high concentrations, β-sheet structure may form, leading to aggregation and precipitation. The storage concentration needs to be controlled (≤ 1 mg/mL).
Biological Activity and Chemical Properties Correlation
Receptor Binding Specificity
Apelin-13 acts through the G protein-coupled receptor APJ. The C-terminal Phe residue is crucial for receptor binding, and N-terminal modifications (such as Pyr) may affect the binding kinetics.
Signal Pathway Activation
After activating the APJ receptor, it inhibits adenylate cyclase (AC) through Gαi/o protein, and simultaneously activates the PI3K/Akt and MAPK/ERK pathways, regulating cardiovascular function, metabolism, and neuroprotection.
Structure-Activity Relationship (SAR)
Shortening the peptide chain (such as Apelin-12) or replacing key residues (such as Phe → Ala) significantly reduces activity, indicating that the complete sequence is crucial for functional maintenance.
FAQ
What is apelin-13?
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Apelin-13 is a 13 amino acid oligopeptide which is the ligand for the apelin receptor (also known as the APJ receptor). It exhibits hypotensive and neuroprotective effects, and may be a potential prognostic biomarker for acute ischemic stroke and multiple sclerosis.
What is the effect of apelin-13 on anxiety like behavior in male rats?
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Conclusion: The results of the study indicate that apelin-13 infusion may lead to a decrease in anxiety-related behaviors in male rats.
What are the benefits of apelin?
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The system is a particularly appealing target for cardiovascular disease as it promotes endothelium-dependent vasodilatation, inotropy, lowers blood pressure, and increases aqueous diuresis. Activating the apelin system also has metabolic and renal benefits.
Is apelin a peptide?
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Apelin is a peptide whose most bioactive form appears to be a 13 amino acid long pyroglutamylated cleavage product from a 77 amino acid precursor (Tatemoto et al., 1998).
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