Endothelin 1 (human, porcine)
Purity: ≥95%
Biological Activity
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
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.
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.
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
(Modifications: Disulfide bridges 1-15, 3-11)
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.
Background References
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Spinal Functions of B-Type Natriuretic Peptide, Gastrin-Releasing Peptide, and Their Cognate Receptors for Regulating Itch in Mice
N Kiguchi, DD Sukhtankar, H Ding, K Tanaka, S Kishioka, CM Peters, MC Ko
J. Pharmacol. Exp. Ther, 2016;356(3):596-603. -
DanHong injection targets endothelin receptor type B and angiotensin II receptor type 1 in protection against cardiac hypertrophy
MY Zhang, FF Guo, HW Wu, YY Yu, JY Wei, SF Wang, YX Zhang, MH Xian, QH Wu, BC Zhao, SY Li, HJ Yang
Oncotarget, 2017;8(61):103393-103409. -
The human endothelin family: three structurally and pharmacologically distinct isopeptides predicted by three separate genes.
Inoue et al.
Proc.Natl.Acad.Sci.U.S.A., 1989;86:2863 -
Involvement of ETA and ETB receptors in the activation of phospholipase D by endothelins in cultured rat cortical astrocytes.
Servitja et al.
Br.J.Pharmacol., 1998;124:1728 -
Primary structure, synthesis, and biological activity of rat endothelin, and endothelium-derived vasoconstrictor peptide.
Yanagisawa et al.
Proc.Natl.Acad.Sci.U.S.A., 1988;85:6964 -
Molecular biology and biochemistry of the endothelins.
Yanagisawa and Masaski
TiPS, 1989;10:374
Product Datasheets
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Citations for Endothelin 1 (human, porcine)
The citations listed below are publications that use Tocris products. Selected citations for Endothelin 1 (human, porcine) include:
16 Citations: Showing 1 - 10
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The role of Nav1.7 and methylglyoxal-mediated activation of TRPA1 in itch and hypoalgesia in a murine model of type 1 diabetes.
Authors: Cheng Et al.
Theranostics 2019;9:4287
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S-nitrosation impairs KLF4 activity and instigates endothelial dysfunction in pulmonary arterial hypertension.
Authors: Ban Et al.
Redox Biol 2019;21:101099
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Fasudil preserves lung endothelial function and reduces pulmonary vascular remodeling in a rat model of end-stage pulmonary hypertension with left heart disease.
Authors: Zhuang Et al.
Int J Mol Med 2018;42:1341
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Dynamics and Functional Role of Dopaminergic Neurons in the Ventral Tegmental Area during Itch Processing.
Authors: Yuan Et al.
J Neurosci 2018;38:9856
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Gastrodin Inhibits Store-Operated Ca(2+) Entry and Alleviates Cardiac Hypertrophy.
Authors: Zheng Et al.
Front Pharmacol 2017;8:222
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IL-11 is a crucial determinant of cardiovascular fibrosis.
Authors: Schafer Et al.
Nature 2017;552:110
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Endothelial cells enhance the migration of bovine meniscus cells.
Authors: Yuan Et al.
J Neurosci 2015;67:182
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The role of K+ and Cl- channels in the regulation of retinal arteriolar tone and blood flow.
Authors: Needham Et al.
J Pharmacol Exp Ther 2014;55:2157
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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.
Authors: Sánchez Et al.
Br J Pharmacol 2014;171:5682
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UV light activates a Gαq/11-coupled phototransduction pathway in human melanocytes.
Authors: Bellono Et al.
J Gen Physiol 2014;143:203
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Inflammatory mediators alter the astrocyte transcriptome and calcium signaling elicited by multiple G-protein-coupled receptors.
Authors: Hamby Et al.
Invest Ophthalmol Vis Sci 2012;32:14489
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Quercetin and its major metabolites selectively modulate cyclic GMP-dependent relaxations and associated tolerance in pig isolated coronary artery.
Authors: Suri Et al.
Br J Pharmacol 2010;159:566
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Interleukin-10 attenuates vascular responses to endothelin-1 via effects on ERK1/2-dependent pathway.
Authors: Giachini Et al.
Am J Physiol Heart Circ Physiol 2009;296:H489
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Endothelin-1 activates ETA receptors to cause reflex scratching in BALB/c mice.
Authors: McQueen Et al.
Br J Pharmacol 2007;151:278
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Pharmacological characterization of endothelin receptors-mediated contraction in the mouse isolated proximal and distal colon.
Authors: Khan Et al.
Br J Pharmacol 2006;147:607
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Involvement of β 3-adrenergic receptor activation via cyclic GMP- but not NO-dependent mechanisms in human corpus cavernosum function.
Authors: Cirino Et al.
Arthritis Rheumatol 2003;100:5531
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