| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
IC50: 0.37 nM (APJ)[1]
APJ receptor (apelin receptor), a class A G protein-coupled receptor (GPCR) closely related to the angiotensin II type 1 receptor. Apelin-13 binds to APJ with high affinity and activates downstream signaling pathways including Galphai-mediated inhibition of cAMP, beta-arrestin recruitment, and MAPK/ERK activation. |
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| ln Vitro |
Apelin-13 is the endogenous ligand of the APJ receptor, activating this GPCR with an EC₅0 value of 0.37 nM. It stimulates high-affinity GTPase activity in APJ-expressing cell membranes. It also induces vasodilation in isolated blood vessels (aorta and arteries) in an endothelium-dependent manner.
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| ln Vivo |
Apelin-13 (200 μg/kg; IP, once day for 4 weeks) dramatically lowers serum levels of TNF-α and leptin, enhances lipid metabolism, strengthens cardiac function, and reduces insulin resistance. increases the levels of GLUT4 and p-AMPKα2 and stimulates the expression of Apelin-12 in serum[2]. ?Most pallidal neurons exhibit an increase in spontaneous discharges when exposed to a single dosage of Apelin-13 (10 and 100 μM; ICV)[4].
Apelin-13 has potent vasodilator and hypotensive effects in vivo, lowering mean arterial blood pressure. It also has a positive inotropic effect on cardiac contractility. In metabolic studies, apelin-13 improves insulin sensitivity and glucose uptake. Microinjection into the dorsal vagal complex reduces gastric tone and motility in a dose-dependent manner via the vagal cholinergic pathway. |
| Enzyme Assay |
Receptor binding assays: Membranes from APJ-transfected HEK293 cells are incubated with [¹2⁵I]-apelin-13 and varying concentrations of unlabeled Apelin-13 TFA. Bound radioactivity is measured after filtration. GTPgammaS binding assays measure receptor activation: membranes are incubated with [3⁵S]-GTPgammaS and apelin-13; bound radioactivity reflects G protein activation.
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| Cell Assay |
APJ-expressing cells (e.g., HEK293-APJ, HUVECs) are treated with Apelin-13 TFA (0.1-100 nM). cAMP levels are measured by competition ELISA (decrease indicates Galphai activation). ERK1/2 phosphorylation is detected by Western blot. Endothelial cells are used to measure nitric oxide production (by Griess assay or DAF-FM fluorescence) and tube formation in Matrigel.
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| Animal Protocol |
Animal/Disease Models: Goto-Kakizaki (GK) rats (12 weeks old; 240-280 g; fed with a high-fat diet: 66.5% standard chow, 10% lard, 20% sucrose, 2.5% cholesterol and 1% pig bile salt)[2]
Doses: 200 µg/kg Route of Administration: IP, daily for 4 weeks Experimental Results: Dramatically diminished heart rate; lowered the levels of fasting plasma glucose (FPG), fasting insulin (FINS) and homeostasis model assessment for insulin resistance (HOMA-IR); diminished serum levels of total cholesterol (TC), triglyceride (TG) and low density lipoprotein-cholesterol (LDL-C) and increased high density lipoprotein-cholesterol (HDL-C); diminished NO level, cNOS activity, TNF-α and leptin in serum; induced the expression of Apelin-12. Animal/Disease Models: Adult Wistar rats (SPF, 8-10 weeks, 240-280 g)[4] Doses: 10 and 100 μM Route of Administration: ICV, single dosage Experimental Results: Increased the spontaneous discharges in the majority of pallidal neurons. In rodents, Apelin-13 TFA is administered intravenously (e.g., 10-100 nmol/kg) to measure acute cardiovascular effects (blood pressure, heart rate). For central effects, microinjection into the dorsal vagal complex (DVC) of anesthetized rats (nmol doses) reduces gastric tone and motility. Metabolic effects are studied in diabetic mouse models. |
| ADME/Pharmacokinetics |
As a 13-amino-acid peptide, Apelin-13 has a very short plasma half-life (<5 minutes) due to rapid degradation by proteases, primarily aminopeptidases. It is cleared quickly from circulation and does not achieve sustained systemic exposure. For in vivo studies, continuous infusion or repeated dosing is required.
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| Toxicity/Toxicokinetics |
No significant toxicity has been reported at research doses (nmol to low micromol range). Apelin-13 is an endogenous peptide, and acute administration is well-tolerated in animal models. No long-term toxicology studies are available. Standard safety precautions for handling peptides apply.
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| References |
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| Additional Infomation |
Apelin-13 is the most potent member of the apelin peptide family (which includes apelin-12, -17, and -36). It is a 13-residue pyroglutamylated peptide derived from the C-terminal region of the 77-amino acid preproapelin. Not FDA-approved; strictly for research use in cardiovascular and metabolic studies.
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| Molecular Formula |
C71H112F3N23O18S
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|---|---|
| Molecular Weight |
1664.85
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| Related CAS # |
Apelin-13;217082-58-1
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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 :~50 mg/mL (~30.03 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (60.07 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 | 0.6007 mL | 3.0033 mL | 6.0065 mL | |
| 5 mM | 0.1201 mL | 0.6007 mL | 1.2013 mL | |
| 10 mM | 0.0601 mL | 0.3003 mL | 0.6007 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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