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Merck
CN

E9137

内皮素 3 人，大鼠

≥97% (HPLC), powder

别名:

ET-3

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关于此项目

经验公式（希尔记法）:
C121H168N26O33S4
化学文摘社编号:
117399-93-6
分子量:
2643.04
NACRES:
NA.32
PubChem Substance ID:
24894690
UNSPSC Code:
12352200
MDL number:
MFCD00076378

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产品名称

内皮素 3 人，大鼠, ≥97% (HPLC), powder

InChI key

OQGZWNZGVYLIFX-XKIQDWPYSA-N

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

assay

≥97% (HPLC)

form

powder

composition

Peptide content, ≥60%

color

white

UniProt accession no.

P13207
P14138

storage temp.

−20°C

Quality Level

200

Gene Information

human ... EDN3(1908)
rat ... Edn3(366270)

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Application

Endothelin 3 has also been used as a ligand for endothelin receptor type B (EDNRB) in ex vivo enteric NCC (eNCC) migration assays.
Endothelin 3 human, rat has been used for culturing neural tube explant culture, and the pharmacological study of endothelin receptors.

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. In mice, it is essential for the development of pigment cells derived from neural crest (NC). Its expression is de-regulated in metastatic melanoma.
Potent vasoconstrictor from vascular endothelial cells.
Potent vasoconstrictor from vascular endothelial cells; preferred agonist for ETB endothelin receptors. Induces the production of VEGF.

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.

存储类别

6.1A - Combustible acute toxic Cat. 1 and 2 / very toxic hazardous materials

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

法规信息

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分析证书(COA)

Lot/Batch Number
0000493644
0000493644
0000354192
0000346318
0000354192

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Juliano T Freitas et al.
Pigment cell & melanoma research, 34(6), 1084-1093 (2021-07-22)
Endothelins are cytokines expressed in the microenvironment of several tumors. To identify which stromal cells in the melanoma microenvironment respond to endothelin, we injected murine melanoma cell lines B16F10, YUMM1.7, and YUMMER1.7 in a transgenic mouse that overexpresses endothelin 3
V T Yeung et al.
Journal of neuroscience research, 46(6), 686-696 (1996-12-15)
The effect of endothelin-3 (ET-3) on cyclic GMP (cGMP) responses to C-type natriuretic peptide (CNP) was studied in primary cultures of mouse astrocytes. Attenuation of CNP-stimulated cGMP formation by ET-3 was time-dependent, with maximum inhibition achieved at 30 min of
J Desmarets et al.
Biochemical and biophysical research communications, 256(2), 357-360 (1999-03-18)
Pharmacological evidence has suggested that endothelin-3 (ET-3) may act via a novel form of ET receptor that is shared by ETA receptor antagonists but not by ETB receptor selective agonists. This study analyses the properties of interaction of ET-3 with
Xiang-jie An et al.
Journal of Huazhong University of Science and Technology. Medical sciences = Hua zhong ke ji da xue xue bao. Yi xue Ying De wen ban = Huazhong keji daxue xuebao. Yixue Yingdewen ban, 33(4), 581-586 (2013-08-02)
Endothelin-3 (ET-3) is aberrantly expressed in both metastatic melanoma tissues and cultured melanoma cells. Our previous work showed that ET-3 could promote survival of metastatic melanoma cells via its altered expression. In this study, we investigated the mechanisms responsible for
E Dupin et al.
Proceedings of the National Academy of Sciences of the United States of America, 97(14), 7882-7887 (2000-07-08)
Functional signaling of endothelin 3 (ET3) and its receptor B (ETRB) has been shown to be required for the development of neural crest (NC)-derived pigment cells in mouse, but the precise role of ET3 is not completely understood. Using the
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