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117399-93-6

117399-93-6 structure
117399-93-6 structure
  • Name: Endothelin-3 (human, mouse, rabbit, rat) acetate salt
  • Chemical Name: Endothelin 3 human, rat
  • CAS Number: 117399-93-6
  • Molecular Formula: C121H168N26O33S4
  • Molecular Weight: 2643.04000
  • Catalog: Biochemical Peptide
  • Create Date: 2018-07-11 21:43:36
  • Modify Date: 2024-01-05 19:54:49
  • 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.

Name Endothelin 3 human, rat
Synonyms ET-3
MFCD00076378
Endothelin 3 human,rat
Endothelin-3, human
Endothelin-3, human, mouse, rabbit, rat
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
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.

Molecular Formula C121H168N26O33S4
Molecular Weight 2643.04000
Exact Mass 2641.11000
PSA 1056.08000
LogP 6.33930
Appearance powder | white
Storage condition −20°C
Safety Phrases S22
RIDADR NONH for all modes of transport
WGK Germany 3