| CAS NO: | 117399-93-6 |
| 生物活性 | Endothelin-3, human, mouse, rabbit, rat is a 21-amino acid vasoactive peptide that binds to G-protein-linked transmembrane receptors,ET-RAandET-RB. | ||||||||||||||||||||
| IC50& Target | ET-RA, ET-RB[1] | ||||||||||||||||||||
| 体外研究 (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]. | ||||||||||||||||||||
| 体内研究 (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]. | ||||||||||||||||||||
| 分子量 | 2643.04 | ||||||||||||||||||||
| Formula | C121H168N26O33S4 | ||||||||||||||||||||
| CAS 号 | 117399-93-6 | ||||||||||||||||||||
| Sequence | 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) | ||||||||||||||||||||
| Sequence Shortening | CTCFTYKDKECVYYCHLDIIW(Disulfide bridge: Cys1-Cys15, Cys3-Cys11) | ||||||||||||||||||||
| 运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||||||
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. | ||||||||||||||||||||
| Solvent & Solubility | In Vitro: H2O Peptide Solubility and Storage Guidelines: 1. Calculate the length of the peptide. 2. Calculate the overall charge of the entire peptide according to the following table:
3. Recommended solution:
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