Endothelin 1 (human, porcine)

Catalog # Availability Size / Price Qty
1160/100U
Endothelin 1 (human, porcine)
4 Images
Description: Potent vasoconstrictor peptide
Alternative Names: ET-1

Purity: ≥95%

Product Details
Citations (16)
Supplemental Products
Reviews

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

Multiplex Immunoassay cardiac hypertrophy assay View Larger

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.

Western Blot western blot and ELISA ANP expression in cardiomyocytes derived from iPSCs View Larger

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

M.Wt:
2492
Formula:
C109H159O32N25S5
Sequence:
CSCSSLMDKECVYFCHLDIIW

(Modifications: Disulfide bridges 1-15, 3-11)

Solubility:
Soluble to 1 mg/ml in water
Purity:
≥95%
Storage:
Store at -20°C
CAS No:
117399-94-7

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

  1. 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.
  2. 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.
  3. 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
  4. 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
  5. 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
  6. Molecular biology and biochemistry of the endothelins.
    Yanagisawa and Masaski
    TiPS, 1989;10:374

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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

  1. 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
  2. S-nitrosation impairs KLF4 activity and instigates endothelial dysfunction in pulmonary arterial hypertension.
    Authors: Ban Et al.
    Redox Biol  2019;21:101099
  3. 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
  4. Dynamics and Functional Role of Dopaminergic Neurons in the Ventral Tegmental Area during Itch Processing.
    Authors: Yuan Et al.
    J Neurosci  2018;38:9856
  5. Gastrodin Inhibits Store-Operated Ca(2+) Entry and Alleviates Cardiac Hypertrophy.
    Authors: Zheng Et al.
    Front Pharmacol  2017;8:222
  6. IL-11 is a crucial determinant of cardiovascular fibrosis.
    Authors: Schafer Et al.
    Nature  2017;552:110
  7. Endothelial cells enhance the migration of bovine meniscus cells.
    Authors: Yuan Et al.
    J Neurosci  2015;67:182
  8. 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
  9. 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
  10. 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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