CAS 117399-93-6|Endothelin-3 (human, mouse, rabbit, rat) acetate salt
| Common Name | Endothelin-3 (human, mouse, rabbit, rat) acetate salt | ||
|---|---|---|---|
| CAS Number | 117399-93-6 | Molecular Weight | 2643.04000 |
| Density | / | Boiling Point | / |
| Molecular Formula | C121H168N26O33S4 | Melting Point | / |
| MSDS | USA | Flash Point | / |
Names
| Name | Endothelin 3 human, rat |
|---|---|
| Synonym | More Synonyms |
BiologicalActivity
| 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 >>OthersPeptidesResearch Areas >>Cardiovascular DiseaseResearch 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. |
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 |
| InChIKey | OQGZWNZGVYLIFX-JQWUVQPESA-N |
| SMILES | CCC(C)C(NC(=O)C(CC(=O)O)NC(=O)C(CC(C)C)NC(=O)C(Cc1c[nH]cn1)NC(=O)C1CSSCC(N)C(=O)NC(C(C)O)C(=O)NC2CSSCC(NC(=O)C(CCC(=O)O)NC(=O)C(CCCCN)NC(=O)C(CC(=O)O)NC(=O)C(CCCCN)NC(=O)C(Cc3ccc(O)cc3)NC(=O)C(C(C)O)NC(=O)C(Cc3ccccc3)NC2=O)C(=O)NC(C(C)C)C(=O)NC(Cc2ccc(O)cc2)C(=O)NC(Cc2ccc(O)cc2)C(=O)N1)C(=O)NC(C(=O)NC(Cc1c[nH]c2ccccc12)C(=O)O)C(C)CC |
| Storage condition | −20°C |
Safety Information
| Safety Phrases | S22 |
|---|---|
| RIDADR | NONH for all modes of transport |
| WGK Germany | 3 |
Articles14
More 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... |
Synonyms
| ET-3 |
| MFCD00076378 |
| Endothelin 3 human,rat |
| Endothelin-3, human |
| Endothelin-3, human, mouse, rabbit, rat |
