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| 1mg |
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| 10mg |
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| Targets |
Apelin receptor (APJ, APLNR), a G protein-coupled receptor (GPCR) belonging to the class A family. APJ is widely expressed in the cardiovascular system, central nervous system, adipose tissue, and other organs. Activation of APJ by apelin peptides leads to Galphai/o-mediated signaling, including inhibition of cAMP production, activation of the PI3K/AKT pathway, and recruitment of beta-arrestin. Apelin-APJ signaling promotes vasodilation, increases cardiac contractility, reduces blood pressure, regulates fluid balance, and modulates glucose and lipid metabolism.
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| ln Vitro |
A radioligand binding assay is performed to determine receptor affinity. Membranes from CHO or HEK293 cells stably expressing the human APJ receptor are incubated with [125I]-Apelin-13 (50 pM) and varying concentrations of (Ala13)-Apelin-13 (0.01 nM to 1 uM) in binding buffer (50 mM HEPES, 5 mM MgCl2, 1 mM CaCl2, 0.5% BSA, pH 7.4) at 25degC for 60-90 minutes. Bound and free radioligand are separated by rapid filtration through GF/B filters. Radioactivity is counted, and Ki values are calculated. (Ala13)-Apelin-13 is an antagonist or partial agonist at APJ.
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| ln Vivo |
In a dose-dependent way, (Ala13)-Apelin-13 TFA (1-300 pmol/60 nl; microinjected into DVC) decreases stomach tone and motility in rats [1].
A functional cAMP inhibition assay (GI pathway) is performed. CHO or HEK293 cells stably expressing human APJ receptor are seeded in 96-well plates and pre-incubated with 1 mM IBMX (phosphodiesterase inhibitor) for 30 minutes. To measure antagonist activity, cells are treated with varying concentrations of (Ala13)-Apelin-13 (0.1 nM to 1 uM) in the presence of a fixed concentration of Apelin-13 (10-100 nM) and forskolin (0.1-1 uM). After 30 minutes, cAMP levels in cell lysates are measured using a competitive ELISA or HTRF-based kit (Cisbio). The EC50 for antagonism is calculated. For beta-arrestin recruitment assays, PathHunter (DiscoverX) or BRET-based assays are used to measure G protein-independent signaling. |
| Enzyme Assay |
For in vitro functional assays, the activity of Apelin-13 analogs is assessed. In cell-based functional assays, (Ala13)-Apelin-13 may act as an antagonist or partial agonist depending on the specific substitution. The full endogenous Apelin-13 peptide activates APJ signaling with EC50 in the low nanomolar range (0.1-5 nM). Substitutions at the C-terminal phenylalanine (position 13) are known to modulate receptor activity and selectivity. Researchers should consult the product datasheet or original literature for specific EC50/IC50 values for (Ala13)-Apelin-13.
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| Cell Assay |
In vivo, Apelin-13 analogs have been used to study APJ signaling in cardiovascular and metabolic regulation. In normotensive and hypertensive rodents, intravenous administration of Apelin-13 (0.1-10 nmol/kg) produces transient, dose-dependent vasodilation and lowers mean arterial pressure (MAP). Apelin-13 also increases cardiac contractility and stroke volume. In contrast, APJ antagonists like (Ala13)-Apelin-13 block these cardiovascular effects. This compound is used as a tool to study APJ pharmacology and to investigate the therapeutic potential of APJ modulation in heart failure, hypertension, and metabolic diseases.
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| Animal Protocol |
For cardiovascular studies, male Sprague-Dawley rats or C57BL/6 mice are anesthetized (isoflurane or ketamine/xylazine). The carotid artery is cannulated for blood pressure and heart rate monitoring (PowerLab system). The jugular vein is cannulated for intravenous drug administration. (Ala13)-Apelin-13 is administered as an intravenous bolus (0.1-10 mg/kg) or as an infusion. To assess antagonist activity, the peptide is administered 5-10 minutes before Apelin-13 challenge. Hemodynamic parameters (MAP, heart rate, left ventricular pressure if a LV catheter is placed) are recorded continuously. Blood samples are collected for plasma analysis of Apelin-13 concentrations (ELISA) and for assessment of renal function (creatinine, BUN) if needed.
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| ADME/Pharmacokinetics |
As a 13-amino acid peptide, Apelin-13 analogs have low oral bioavailability (typically <1%) due to proteolytic degradation in the gastrointestinal tract. In pharmacokinetic studies, Apelin-13 administered intravenously (IV) shows a very short half-life of 2-8 minutes in rodents due to rapid degradation by peptidases (particularly angiotensin-converting enzyme 2, ACE2) and renal clearance. The volume of distribution is moderate (0.5-1.5 L/kg), indicating distribution into tissues. For research purposes, peptides are typically administered IV or intraperitoneally (IP). The TFA salt form is used to improve solubility and stability during storage.
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| Toxicity/Toxicokinetics |
As an endogenous peptide analog, (Ala13)-Apelin-13 is generally well-tolerated at the concentrations used in research. The full Apelin-13 peptide has no significant toxicity in preclinical studies. Acute administration of Apelin-13 in rodents at doses up to 10 mg/kg IV or 30 mg/kg IP does not cause mortality, significant changes in body weight, or organ toxicity (liver, kidney). No genotoxicity or immunogenicity has been reported for Apelin peptides. The TFA counterion is non-toxic at low concentrations. Standard safety precautions for handling synthetic peptides apply.
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| References |
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| Additional Infomation |
The apelin-APJ system is an attractive therapeutic target for cardiovascular diseases, including heart failure (HF). In heart failure, apelin levels are reduced, and APJ agonists are being developed to improve cardiac contractility and reduce afterload without the adverse effects of other inotropes. Several apelin analogs and small-molecule APJ agonists have entered clinical trials for heart failure (e.g., Apelin-17 derivative). (Ala13)-Apelin-13 is a research tool for APJ pharmacology, allowing researchers to study the specific role of the C-terminal phenylalanine in receptor activation. This product is for research use only and is not FDA-approved for human therapy.
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| Molecular Formula |
C63H107N23O16S.XC2HF3O2
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| Molecular Weight |
1474.73 (free acid)
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| Related CAS # |
(Ala13)-Apelin-13;568565-11-7
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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
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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.) |
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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