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Submit ReviewEndothelin 1 (human, porcine)
Description: Potent vasoconstrictor peptide
Alternative Names: ET-1
Purity: ≥95% (HPLC)
Biological Activity for Endothelin 1 (human, porcine)
Endothelin 1 (human, porcine) is a potent endogenous peptide agonist at ETA and ETB receptors. Produces strong vasoconstriction and pressor responses. Competitive binding assay shows that Endothelin 1 reversibly binds to receptors (IC50 values are 0.12 nM and 0.15 nM at ETB and ETA receptors respectively). Potency is dependent on blood vessel type (EC50 ranges from 2.72 nM - 17.4 nM). Activates PLC (EC50 = 0.3 nM), increases production of PGE2 (EC50 = 12 nM) and induces intracellular calcium release in human ciliary muscle cells. Also upregulates leptin mRNA expression and secretion in adipocytes (EC50 = 8.8 nM).
Scientific Data
Multiplex Immunoassay
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Pluripotent stem cell-derived cardiomyocytes secrete Pro-BNP in response to small molecule-induction of cardiac hypertrophy Cardiomyocytes were treated with the vasoconstrictor, ET-1 (Endothelin-1; Catalog # 1160), or one of two L-type calcium channel inhibitors, Doxorubicin (Catalog # 2252) or Verapamil (Catalog # 0654). Levels of the cardiac hypertrophy marker, Pro-Brain Natriuretic Peptide (Pro-BNP), were detected via Luminex® bead-based multiplex assay (Catalog # LXSAH). A substantial increase in Pro-BNP was detected in the medium of cardiomyocytes treated with ET-1, a known inducer of cardiac hypertrophy. Conversely, Doxorubicin and Verapamil decreased Pro-BNP secretion from cardiomyocytes.
ELISA
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Differentiated cardiomyocytes respond physiologically to Endothelin-1 induced hypertrophy Cardiomyocytes differentiated from BG01V human embryonic stem cells were treated with Endothelin-1 (ET-1; Catalog # 1160) for 28 hours to induce cardiac hypertrophy. Levels of Pro-Atrial Natriuretic peptide (Pro-ANP) secretion, which is known to be elevated during cardiac hypertrophy, were assessed using ELISA (Catalog # DANP00). As expected, detection of Pro-ANP increased proportionally with the concentration of Endothelin-1 treatment.
Western Blot
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Endothelin Induces Expression of Atrial Natriuretic Peptide in Cardiomyocytes Derived from iPSCs JOY6 human iPSCs were differentiated into beating cardiomyocytes. After 21 days of differentiation cardiomyocytes were treated with 5 nM of Endothelin-1 (ET-1; Catalog # 1160) for 25.5 hours to induce cardiac hypertrophy. The level of secreted Pro-Atrial Natriuretic peptide (Pro-ANP), which is known to be elevated during cardiac hypertrophy, was assessed using (A) Western Blot and (B) ELISA (Human NTProANP Quantikine® ELISA; Catalog # DANP00). As expected, detection of Pro-ANP was increased in Endothelin-1 treated cells.
Technical Data for Endothelin 1 (human, porcine)
| M. Wt | 2492 |
| Formula | C109H159O32N25S5 |
| Sequence |
CSCSSLMDKECVYFCHLDIIW (Modifications: Disulfide bridges 1-15, 3-11) |
| Storage | Store at -20°C |
| Purity | ≥95% (HPLC) |
| CAS Number | 117399-94-7 |
| PubChem ID | 16133807 |
| InChI Key | ZUBDGKVDJUIMQQ-ZTNLKOGPSA-N |
| Smiles | [H][C@](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC1=CNC=N1)NC(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](CO)C(=O)N[C@@]2([H])CSSC[C@]([H])(NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC2=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC2=CC=C(O)C=C2)C(=O)N[C@H](CC2=CC=CC=C2)C(=O)N1)([C@@H](C)CC)C(=O)N[C@@]([H])([C@@H](C)CC)C(=O)N[C@@H](CC1=CNC2=C1C=CC=C2)C(O)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Endothelin 1 (human, porcine)
| Solubility | Soluble to 1 mg/ml in water |
Product Datasheets for Endothelin 1 (human, porcine)
References for Endothelin 1 (human, porcine)
References are publications that support the biological activity of the product.
Inoue et al (1989) The human endothelin family: three structurally and pharmacologically distinct isopeptides predicted by three separate genes. Proc.Natl.Acad.Sci.U.S.A. 86 2863 PMID: 2649896
Servitja et al (1998) Involvement of ETA and ETB receptors in the activation of phospholipase D by endothelins in cultured rat cortical astrocytes. Br.J.Pharmacol. 124 1728 PMID: 9756390
Yanagisawa et al (1988) Primary structure, synthesis, and biological activity of rat endothelin, and endothelium-derived vasoconstrictor peptide. Proc.Natl.Acad.Sci.U.S.A. 85 6964 PMID: 3045827
Yanagisawa and Masaski (1989) Molecular biology and biochemistry of the endothelins. TiPS 10 374 PMID: 2690429
Matsumoto et al (1996) Endothelin-induced changes of second messengers in cultured human ciliary muscle cells Invest.Ophthalmol.Vis.Sci. 37 1058 PMID: 8631621
Xiong et al (2001) Endothelin-1 stimulates leptin production in adipocytes. J.Biol.Chem. 276 28471 PMID: 11359784
Maguire and Davenport et al (1995) ETA receptor-mediated constrictor responses to endothelin peptides in human blood vessels in vitro. Br.J.Pharmacol. 115 191 PMID: 7647976
If you know of a relevant reference for Endothelin 1 (human, porcine), please let us know.
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Keywords: Endothelin 1 (human, porcine), Endothelin 1 (human, porcine) supplier, Potent, vasoconstrictor, peptide, Endothelin, Non-Selective, ET, Receptors, agonists, Endothelin1, (human, porcine), presoor, blood, pressure, vein, artery, PLC, phospholipase, C, prostagladin, PGE, PGE2, intracellular, calcium, leptin, adipocytes, ET-1, Non-selective, Phospholipases, 1160, Tocris Bioscience
16 Citations for Endothelin 1 (human, porcine)
Citations are publications that use Tocris products. Selected citations for Endothelin 1 (human, porcine) include:
Yuan et al (2018) Dynamics and Functional Role of Dopaminergic Neurons in the Ventral Tegmental Area during Itch Processing. J Neurosci 38 9856 PMID: 30266741
Zhuang et al (2018) Fasudil preserves lung endothelial function and reduces pulmonary vascular remodeling in a rat model of end-stage pulmonary hypertension with left heart disease. Int J Mol Med 42 1341 PMID: 29901088
Bellono et al (2014) UV light activates a Gαq/11-coupled phototransduction pathway in human melanocytes. J Gen Physiol 143 203 PMID: 24470488
Sánchez et al (2014) Endothelin-1 contributes to endothelial dysfunction and enhanced vasoconstriction through augmented superoxide production in penile arteries from Ins-resistant obese rats: role of ET(A) and ET(B) receptors. Br J Pharmacol 171 5682 PMID: 25091502
Hamby et al (2012) Inflammatory mediators alter the astrocyte transcriptome and calcium signaling elicited by multiple G-protein-coupled receptors. Invest Ophthalmol Vis Sci 32 14489 PMID: 23077035
McQueen et al (2007) Endothelin-1 activates ETA receptors to cause reflex scratching in BALB/c mice. Br J Pharmacol 151 278 PMID: 17351652
Needham et al (2014) The role of K+ and Cl- channels in the regulation of retinal arteriolar tone and blood flow. J Pharmacol Exp Ther 55 2157 PMID: 24609622
Cheng et al (2019) The role of Nav1.7 and methylglyoxal-mediated activation of TRPA1 in itch and hypoalgesia in a murine model of type 1 diabetes. Theranostics 9 4287 PMID: 31285762
Zheng et al (2017) Gastrodin Inhibits Store-Operated Ca(2+) Entry and Alleviates Cardiac Hypertrophy. Front Pharmacol 8 222 PMID: 28487655
Giachini et al (2009) Interleukin-10 attenuates vascular responses to endothelin-1 via effects on ERK1/2-dependent pathway. Am J Physiol Heart Circ Physiol 296 H489 PMID: 19074677
Cirino et al (2003) Involvement of β 3-adrenergic receptor activation via cyclic GMP- but not NO-dependent mechanisms in human corpus cavernosum function. Arthritis Rheumatol 100 5531 PMID: 12707413
Schafer et al (2017) IL-11 is a crucial determinant of cardiovascular fibrosis. Nature 552 110 PMID: 29160304
Yuan et al (2015) Endothelial cells enhance the migration of bovine meniscus cells. J Neurosci 67 182 PMID: 25307081
Suri et al (2010) Quercetin and its major metabolites selectively modulate cyclic GMP-dependent relaxations and associated tolerance in pig isolated coronary artery. Br J Pharmacol 159 566 PMID: 20050852
Khan et al (2006) Pharmacological characterization of endothelin receptors-mediated contraction in the mouse isolated proximal and distal colon. Br J Pharmacol 147 607 PMID: 16432510
Ban et al (2019) S-nitrosation impairs KLF4 activity and instigates endothelial dysfunction in pulmonary arterial hypertension. Redox Biol 21 101099 PMID: 30660098
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