Endothelin-3, human, mouse, rabbit, rat  (Synonyms: Endothelin 3 (Rat,Human))

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.

ET-RA, ET-RB^[1]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

2643.04

C₁₂₁H₁₆₈N₂₆O₃₃S₄

117399-93-6

Cys-Thr-Cys-Phe-Thr-Tyr-Lys-Asp-Lys-Glu-Cys-Val-Tyr-Tyr-Cys-His-Leu-Asp-Ile-Ile-Trp(Disulfide bridge: Cys1-Cys15, Cys3-Cys11)

CTCFTYKDKECVYYCHLDIIW(Disulfide bridge: Cys1-Cys15, Cys3-Cys11)

O=C([C@H]1NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@]2([H])NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@](NC([C@@H](NC([C@@](CSSC2)([H])NC([C@](NC([C@H](CSSC1)N)=O)([H])[C@H](O)C)=O)=O)CC3=CC=CC=C3)=O)([H])[C@H](O)C)=O)CC4=CC=C(C=C4)O)=O)CCCCN)=O)CC(O)=O)=O)CCCCN)=O)CCC(O)=O)=O)=O)C(C)C)=O)CC5=CC=C(C=C5)O)=O)CC6=CC=C(C=C6)O)=O)N[C@@H](CC7=CN=CN7)C(N[C@@H](CC(C)C)C(N[C@@H](CC(O)=O)C(N[C@@H]([C@@H](C)CC)C(N[C@@H]([C@@H](C)CC)C(N[C@H](C(O)=O)CC8=CNC9=CC=CC=C89)=O)=O)=O)=O)=O

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Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]