Endothelin-3 (human, mouse, rabbit, rat) acetate salt

Names

[ Name ]:
Endothelin-3 (human, mouse, rabbit, rat) acetate salt

[Synonym ]:
ET-3
MFCD00076378
Endothelin 3 human,rat
Endothelin-3, human
Endothelin-3, human, mouse, rabbit, rat

Biological Activity

[Description]:

Endothelin-3, human, mouse, rabbit, rat is a 21-amino acid vasoactive peptide that binds to G-protein-linked transmembrane receptors, ET-RA and ET-RB.

[Related Catalog]:

Signaling Pathways >> Others >> Others

Peptides

Research Areas >> Cardiovascular Disease

Research Areas >> Neurological Disease

[Target]

ET-RA, ET-RB[1]

[In Vitro]

The endothelins (ETs) are a family of 21-amino-acid vasoconstrictor peptides comprising three distinct isoforms: ET-1, ET2 and Endothelin-3. Endothelin-3 is detected in plasma, heart, brain and vascular smooth muscle cells (VSMCs). The surface enzymes of VSMCs break down big Endothelin-3 to the corresponding mature peptide, Endothelin-3. Endothelin-3 down-regulate endothelin ETA receptor expression in coronary artery VSMCs without affecting receptor density or functional ETA receptor responses. By contrast, high concentrations of Endothelin-3 (100 nM) increase the expression of ETB receptors but abolish the vasoconstrictor response of the receptors, possibly due to the desensitizing effect of Endothelin-3[1]. Endothelin-3 stimulates ENCC adhesion to various ECM components. Endothelin-3 induces rapid changes in ENCC shape and protrusion dynamics favouring sustained growth and stabilization of lamellipodia, a process coincident with the increase in the number of focal adhesions and activated β1-integrins[2].

[In Vivo]

Endothelin-3 at low concentrations may attenuate inflammatory responses via ETB2 activation and NO production. Endothelin-3, which acts mainly on ETB, at low concentrations specifically inhibited platelet-activating factor (PAF)-induced paw oedema, whereas neither ET-1 nor Endothelin-2, both of which act on ETA and ETB, showed inhibitory activity. The inhibition by ET-1 and Endothelin-3 (each 0.5 pmol/paw) in the presence of BQ-123 (66.4 ± 6.7 % and 65.4 ± 22.6 %, respectively), is comparable to that by Endothelin-3 (0.5 pmol/paw) alone (65.4 ± 10.9 %), whereas neither ET-1 nor Endothelin-3 in the presence of BQ-788 showed inhibitory activity[3].

[References]

[1]. Skovsted GF, et al. Endothelin-1 and Endothelin-3 Regulate Endothelin Receptor Expression in Rat Coronary Arteries. Basic Clin Pharmacol Toxicol. 2015 Nov;117(5):297-305.

[2]. Gazquez E, et al. Endothelin-3 stimulates cell adhesion and cooperates with β1-integrins during enteric nervous system ontogenesis. Sci Rep. 2016 Dec 1;6:37877. doi: 10.1038/srep37877.

[3]. Sato A, et al. Endothelin-3 at low concentrations attenuates inflammatory responses via the endothelin B2 receptor. Inflamm Res. 2013 Apr;62(4):417-24.

[Related Small Molecules]

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₂₁H₁₆₈N₂₆O₃₃S₄

[ Molecular Weight ]:
2643.04000

[ Exact Mass ]:
2641.11000

[ PSA ]:
1056.08000

[ LogP ]:
6.33930

[ Appearance of Characters ]:
powder | white

[ Storage condition ]:
−20°C

Safety Information

[ Safety Phrases ]:
S22

[ RIDADR ]:
NONH for all modes of transport

[ WGK Germany ]:
3

Articles

Involvement of endothelins in deoxycorticosterone acetate-salt hypertension through the modulation of noradrenergic transmission in the rat posterior hypothalamus.

Exp. Physiol. 100 , 617-27, (2015)

What is the central question of this study? Does ex vivo administration of endothelin-1 and endothelin-3 regulate noradrenergic transmission in the posterior hypothalamus of deoxycorticosterone acetat...

Direct conversion of mouse and human fibroblasts to functional melanocytes by defined factors.

Nat. Commun. 5 , 5807, (2014)

Direct reprogramming provides a fundamentally new approach for the generation of patient-specific cells. Here, by screening a pool of candidate transcription factors, we identify that a combination of...

Analysis of immunostaining and western blotting of endothelin 1 and its receptors in mitral stenosis.

Rev. Bras. Cir. Cardiovasc. 30 , 211-8, (2015)

Rheumatic Fever represents a serious public health problem in developing countries, with thousands of new cases each year. It is an autoimmune disease, which occurs in response to infection by strepto...