| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
Apelin-17 targets the APJ receptor, an orphan G protein-coupled receptor. It binds to the human APJ receptor expressed in HEK 293 cells with a pIC₅0 of 9.02. The peptide potently inhibits forskolin-stimulated cAMP accumulation with a pIC₅0 of 9.94.
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| ln Vitro |
In vitro, Apelin-17 potently inhibits forskolin-stimulated cAMP accumulation (pIC₅0 = 9.94). It binds to the APJ receptor with high affinity (pIC₅0 = 9.02). The peptide also inhibits the entry of some HIV-1 and HIV-2 strains into NP2/CD4 cells.
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| ln Vivo |
In vivo, Apelin-17 is a potent diuretic neuropeptide that counteracts vasopressin actions through inhibition of vasopressin neuron activity and vasopressin release. It is involved in fluid homeostasis and cardiovascular regulation. The peptide is secreted by adipocytes and plays a role in metabolism.
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| Enzyme Assay |
Receptor binding assays for Apelin-17 use membrane preparations from cells expressing the APJ receptor. Radiolabeled apelin is incubated with varying concentrations of the test peptide, and binding affinity (pIC₅0) is determined from competition binding curves.
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| Cell Assay |
Cellular assays for Apelin-17 typically use cell lines expressing the APJ receptor. Cells are treated with the peptide, and cAMP accumulation is measured to assess receptor activation. HIV-1 entry inhibition assays can also be performed.
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| Animal Protocol |
In vivo studies with Apelin-17 are conducted in rodent models. The peptide is typically administered via intravenous or intracerebroventricular injection. Diuretic effects, vasopressin levels, and fluid balance are assessed.
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| ADME/Pharmacokinetics |
As a 17-amino acid peptide, Apelin-17 is expected to have a short half-life due to proteolytic degradation. The peptide is soluble in water up to 1.20 mg/mL and should be stored desiccated at -20degC.
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| Toxicity/Toxicokinetics |
Toxicity data for Apelin-17 are limited. Peptide research compounds are generally considered to have low toxicity at pharmacological doses. Standard safety precautions for laboratory handling of peptides should be followed.
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| References |
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| Additional Infomation |
Apelin-17 is a research-use peptide and is not approved for therapeutic applications. It is available for human and bovine research. The peptide is used to study the apelin/APJ system, fluid homeostasis, cardiovascular function, and metabolism. It is available from multiple research suppliers.
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| Molecular Formula |
C96H156N34O20S
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|---|---|
| Molecular Weight |
2138.5467
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| Exact Mass |
2137.2
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| CAS # |
217082-57-0
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| Related CAS # |
Apelin-17(human, bovine) TFA
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| Appearance |
White to off-white solid powder
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| LogP |
4.584
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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 : ~100 mg/mL (~46.76 mM)
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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 | 0.4676 mL | 2.3380 mL | 4.6761 mL | |
| 5 mM | 0.0935 mL | 0.4676 mL | 0.9352 mL | |
| 10 mM | 0.0468 mL | 0.2338 mL | 0.4676 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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