| 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 |
Endothelin 1 (swine, human) acts as a potent, endogenous agonist for two main types of G protein-coupled receptors: endothelin receptor A (ETA) and endothelin receptor B (ETB). ETA receptors are primarily located on vascular smooth muscle cells and mediate vasoconstriction and cell proliferation, while ETB receptors are found on endothelial cells and mediate vasodilation through nitric oxide release, as well as acting as clearance receptors. The peptide has proinflammatory and profibrotic effects.
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| ln Vitro |
In vitro, Endothelin 1 is widely used to study its potent vasoconstrictor and mitogenic effects on vascular smooth muscle cells. It is also used in assays to characterize the pharmacological profiles of ETA and ETB receptor antagonists. In cell-based systems, it can stimulate cell proliferation, migration, and the production of extracellular matrix components, which are key processes in vascular remodeling and fibrosis.
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| ln Vivo |
In vivo, Endothelin 1 is a powerful endogenous vasoconstrictor that contributes to the regulation of blood pressure and vascular tone. Its dysregulation is implicated in the pathophysiology of hypertension, pulmonary arterial hypertension, and heart failure. The compound is used in animal models to study these disease states and to evaluate the therapeutic potential of endothelin receptor antagonists.
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| Enzyme Assay |
For non-cellular in vitro enzyme/receptor binding assays, Endothelin 1 is used as the standard ligand in radioligand binding studies to determine the affinity of novel compounds for ETA and ETB receptors. In these assays, the radiolabeled peptide is incubated with membrane preparations from cells expressing the receptors, and its displacement by test compounds is measured to calculate inhibition constants (Ki).
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| Cell Assay |
For in vitro cellular assays, Endothelin 1 is used to stimulate downstream signaling pathways in cells expressing ETA or ETB receptors. A common assay is the measurement of intracellular calcium mobilization, as the receptors are Gq-coupled. Cells are loaded with a calcium-sensitive dye, and the increase in fluorescence upon peptide addition is measured. This assay is used to confirm receptor functionality and to evaluate the agonist or antagonist properties of test compounds.
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| Animal Protocol |
For in vivo animal studies, Endothelin 1 is often administered to rodents via intravenous injection to induce a potent and sustained pressor response, modeling hypertension. It is also used in models of pulmonary hypertension, where chronic infusion can lead to the development of pulmonary vascular remodeling and right heart failure, replicating key features of the human disease. The compound is central to evaluating the efficacy of endothelin receptor antagonists.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Endothelin 1 (swine, human) (TFA) are typically those of the endogenous peptide. It has a very short half-life in the circulation, on the order of minutes, due to rapid clearance by ETB receptors in the lungs and kidneys, as well as degradation by neutral endopeptidase. This rapid clearance is a key feature of its physiology. For research use, it is often administered via continuous infusion to maintain stable plasma concentrations. The TFA salt form enhances its solubility and stability for in vitro and in vivo applications.
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| Toxicity/Toxicokinetics |
Toxicological data for Endothelin 1 are not applicable as it is a research tool, not a therapeutic agent. However, its potent vasoconstrictor activity means that high doses can be life-threatening, causing acute hypertension, myocardial ischemia, and other severe cardiovascular events. Therefore, it must be handled with extreme care in laboratory settings. All research use must strictly adhere to institutional safety protocols for handling potent vasoactive substances.
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| References | |
| Additional Infomation |
Endothelin 1 (swine, human) (TFA) is a 21-amino acid synthetic peptide identical to the endogenous vasoconstrictor. With a molecular weight of 2605.92 and the sequence CSCSSLMDKECVYFCHLDIIW, it acts as an agonist at both ETA and ETB receptors. It is a cornerstone research tool for studying cardiovascular physiology, hypertension, fibrosis, and inflammation.
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| CAS # |
394693-38-0
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| Related CAS # |
Endothelin 1 (swine, human);117399-94-7
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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) |
DMSO: 50 mg/mL (19.19 mM)
H2O: 20 mg/mL (7.67 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.) |
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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