ENDOTHELIN-3
endothelin 3
CAS: 117399-93-6
Molecular Formula: C121H168N26O33S4
ENDOTHELIN-3 - Names and Identifiers
ENDOTHELIN-3 - Physico-chemical Properties
| Molecular Formula | C121H168N26O33S4 |
| Molar Mass | 2643.04 |
| Density | 1.285±0.06 g/cm3(Predicted) |
| Appearance | powder |
| Color | white |
| Storage Condition | −20°C |
| MDL | MFCD00076378 |
| In vitro study | 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. 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. |
| In vivo study | 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. |
ENDOTHELIN-3 - Risk and Safety
| Safety Description | 22 - Do not breathe dust. |
| WGK Germany | 3 |
| FLUKA BRAND F CODES | 3-10 |
ENDOTHELIN-3 - Reference Information
| overview | endothelin is a powerful vasoconstrictor peptide found in porcine aortic endothelial cell culture medium Yanagisawa by Japanese scholars in 1988. it consists of 21 amino acids and is an active polypeptide with the strongest effect and the longest duration in vivo. It is not only a circulating hormone that constricts blood vessels and promotes blood pressure in endothelial cells, but also a potential neurotransmitter and cell growth factor widely distributed in nerve tissue, vascular smooth muscle and macrophages. In addition to vascular endothelial cells, other cells such as neurons, epidermal cells, cardiomyocytes, adrenal glands and other cells can secrete endothelin, and participate in the promotion of cell proliferation and the physiological function regulation of multiple systems in the body in the way of autocrine/paracrine. At present, it is found that there are four isomeric peptides of endothelin -1,2,3(ET-1,ET-2,ET-3) and vasoactive intestinal contractile peptide (vasoactiveintestinalconstrictor,VIC), called "endothelin family". ET-1 is mainly expressed in endothelial cells, ET-2 is more expressed in kidney, endothelin 3 is mainly expressed in nervous system, and VIC is an active polypeptide found in mice that has contractile effect on intestinal smooth muscle. |
| Application | Human endothelin 3 interacts with endothelin receptor B on the cell surface. During the entire embryonic development, EDN3 participates in neural crest cells, which migrate from the developing spinal cord to specific areas in the embryo, where they produce many different types of cells. Human endothelin-3 and EDN3R are necessary for nerve formation in the large intestine (enteric nerve) and melanocytes (which produce melanin). Mutations in the EDN3 gene are associated with Waardenburg syndrome, and type IV is characterized by changes in skin, hair and eye coloration. Mutations in the human endothelin 3 gene are associated with Hirschsprung's disease causing severe constipation or intestinal obstruction. |
| biological activity | Endothelin-3, human, mouse, rabbit, rat is a vasoactive peptide composed of 21 amino acids, which can be connected with G protein Transmembrane receptor, ET-RA and ET-RB binding. |
| target | ET-RA, ET-RB |
Last Update：2024-04-09 20:52:54
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