E9137

Endothelin 3 human, rat

≥97% (HPLC), powder

• Synonym(s): ET-3
• Empirical Formula (Hill Notation): C₁₂₁H₁₆₈N₂₆O₃₃S₄
• CAS Number: 117399-93-6
• Molecular Weight: 2643.04
• MDL number: MFCD00076378
• UNSPSC Code: 12352200
• PubChem Substance ID: 24894690
• NACRES: NA.32

Properties

• Quality Level: 200
• assay: ≥97% (HPLC)
• form: powder
• composition: Peptide content, ≥60%
• color: white
• UniProt accession no.: P13207; P14138
• storage temp.: −20°C
• SMILES string: [H]N[C@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@@H](NC(=O)[C@@H]4CSSC[C@H](NC(=O)[C@@H](NC1=O)[C@H](C)O)C(=O)N[C@@H](Cc5ccccc5)C(=O)N[C@@H]([C@H](C)O)C(=O)N[C@@H](Cc6ccc(O)cc6)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(O)=O)C(=O)N4)C(C)C)C(=O)N[C@@H](Cc7cnc[nH]7)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](Cc8c[nH]c9ccccc89)C(O)=O
• InChI: 1S/C121H168N26O33S4/c1-11-62(7)97(117(175)139-89(121(179)180)49-70-53-126-77-25-17-16-24-75(70)77)145-118(176)98(63(8)12-2)144-112(170)88(52-95(157)158)136-105(163)81(44-60(3)4)131-109(167)86(50-71-54-125-59-127-71)134-113(171)90-56-182-181-55-76(124)101(159)146-99(64(9)148)120(178)142-91-57-183-184-58-92(115(173)143-96(61(5)6)116(174)137-84(48-69-32-38-74(152)39-33-69)107(165)132-82(108(166)141-90)46-67-28-34-72(150)35-29-67)140-104(162)80(40-41-93(153)154)130-102(160)78(26-18-20-42-122)129-110(168)87(51-94(155)156)135-103(161)79(27-19-21-43-123)128-106(164)83(47-68-30-36-73(151)37-31-68)138-119(177)100(65(10)149)147-111(169)85(133-114(91)172)45-66-22-14-13-15-23-66/h13-17,22-25,28-39,53-54,59-65,76,78-92,96-100,126,148-152H,11-12,18-21,26-27,40-52,55-58,122-124H2,1-10H3,(H,125,127)(H,128,164)(H,129,168)(H,130,160)(H,131,167)(H,132,165)(H,133,172)(H,134,171)(H,135,161)(H,136,163)(H,137,174)(H,138,177)(H,139,175)(H,140,162)(H,141,166)(H,142,178)(H,143,173)(H,144,170)(H,145,176)(H,146,159)(H,147,169)(H,153,154)(H,155,156)(H,157,158)(H,179,180)/t62-,63-,64?,65?,76-,78-,79-,80-,81-,82-,83-,84-,85-,86-,87-,88-,89-,90-,91-,92-,96-,97-,98-,99-,100-/m0/s1
• InChI key: OQGZWNZGVYLIFX-XKIQDWPYSA-N
• Gene Information: human ... EDN3(1908) ; rat ... Edn3(366270)

Description

Amino Acid Sequence

Cys-Thr-Cys-Phe-Thr-Tyr-Lys-Asp-Lys-Glu-Cys-Val-Tyr-Tyr-Cys-His-Leu-Asp-Ile-Ile-Trp [Disulfide Bridges: 1-15; 3-11]

General description

Endothelin 3 (ET3) belongs to endothelin peptide family, which includes three members, ET-1, -2 and -3. These are 21-amino acid peptides, which are synthesized as precursors. They are converted to biologically active peptides, after being cleaved by proteases. There are two endothelin receptors called ETRA and ETRB, and ET3 binds to ETRB. It is localized to human intestine and colon.[1]

Application

Endothelin 3 has also been used as a ligand for endothelin receptor type B (EDNRB) in ex vivo enteric NCC (eNCC) migration assays.[2]

Endothelin 3 human, rat has been used for culturing neural tube explant culture,[3] and the pharmacological study of endothelin receptors.[4]

Biochem/physiol Actions

Endothelin 3 (ET3) is a vasoconstrictor that acts in a paracrine and autocrine manner, and in intestinal lamina propria causes the degranulation of mast cells. It results in the release of ions from intestinal epithelial cells. In acute and chronic intestinal inflammation, it is overexpressed. It is also up-regulated in colon carcinoma, where it supports cell proliferation and survival. It might be involved in colon homeostasis, and is essential for the survival and proliferation of goblet cells.[1] In mice, it is essential for the development of pigment cells derived from neural crest (NC).[5] Its expression is de-regulated in metastatic melanoma.[6]

Potent vasoconstrictor from vascular endothelial cells.

Potent vasoconstrictor from vascular endothelial cells; preferred agonist for ET_B endothelin receptors. Induces the production of VEGF.

Safety Information

• Storage Class: 6.1A - Combustible acute toxic Cat. 1 and 2 / very toxic hazardous materials
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable