Dye-Labeled Endothelins – HiLyte™ Fluor 488 & 5-FAM


Expanding on its world-class collection of Endothelin peptides, AnaSpec is pleased to announce the release of new HiLyte™ Fluor 488 and 5-FAM labeled Endothelin peptides (human, bovine, porcine, rat).

Endothelins (ET) are highly potent vasoconstrictor proteins distributed throughout all areas of the body, and are implicated in a number of conditions and diseases.1 Members of the Endothelin family of peptides consist of Pre-pro-endothelin-1, a biologically inactive precursor form cleaved by furin covertase to produce Big Endothelin-1 (Big ET-1), which is cleaved again by endothelin converting enzyme (ECE) between Trp-21 and Val-22 to yield the active ET-1 (1-21). 2 Alternatively, pulmonary chymase is also capable of generating ET-1 (1-31) by cleaving the Tyr31–Gly32 bond of big ET-1.2, 3 Isoforms include ET-2, ET-3, and ET-4.2 All have two disulfide bonds that hold them in a conical spiral shape.2 In addition to their vasoconstrictive properties, endothelins have inotropic and mitogenic properties.2 They influence salt and water balance, affect intracellular Ca2+ concentrations and signal transduction cascades, contract non-vascular smooth muscle, alter central and peripheral sympathetic activity, and stimulate the renin-angiotensin-aldosterone system.2-5

ETs are normally kept at stable levels in healthy individuals, but can become overexpressed, leading to high blood pressure, kidney disease, and numerous cardiovascular diseases such as pulmonary hypertension, cardiac hypertrophy, myocardial infarction, heart failure, and cerebral vasospasm.1, 2 ET disregulation is also a key component of tumorigenesis in several types of cancer.6

Fluorescently labeled endothelins have various applications in ET-related disease research. They are utilized as probes in visualizing intracellular processes and molecular interactions between ET-1 and potential ET-antagonists or inhibitors at the cellular level.7 They are also used for localizing and monitoring ECE activity and ET-receptor binding affinity via fluorescence fluctuation spectroscopy.8, 9 Specific ET isoform binding sites throughout the body may be studied using labeled ET. In addition, flow cytometry is used in combination with labeled ET to assay ET-receptor expression during different periods of the cell cycle, 10 and in vivo and in vitro imaging of ET activity is capable with fluorescent ET.11 Overall, these unique peptides offer a wide range of approaches to further study ET function and ET-related mechanisms.



Table 1. Listing of dye-labeled endothelins.

Product

Size

Catalog #

Big Endothelin-1 (1-38), human, FAM labeled
"FAM-CSCSSLMDKECVYFCHLDIIWVNTPEHVVPYGLGS
PRS (Disulfide bridges Cys 1-15, Cys 3-11)"

0.25 mg

0.5 mg

64825-025

64825-05

Endothelin 1, human, FAM-labeled
FAM-CSCSSLMDKECVYFCHLDIIW
(Disulfide bri dge: 1-15 and 3-11)

0.5 mg

1 mg

27116

27117

Endothelin 2, human, FAM-labeled
FAM-CSCSSWLDKECVYFCHLDIIW
(Disulfide bridge: 1-15 and 3-11)

0.5 mg

1 mg

64536-05

64536-1

Endothelin 3, human, rat, HiLyte™ Fluor 488 labeled
HiLyte™ Fluor 488-CTCFTYKDKECVYYCHLDIIW
(Disulfide bridge: 1-15 and 3-11)

0.25 mg

0.5 mg

64829-025

64829-05

Endothelin 3, human, rat, FAM-labeled
FAM-CTCFTYKDKECVYYCHLDIIW
(Disulfide bridge: 1-15 and 3-11)

0.25 mg

0.5 mg

64816-025

64816-05























Table 2. Listing of endothelins.
Product

Size

Catalog #

Big Endothelin-1 (1-38), human
CSCSSLMDKECVYFCHLDIIWVNTPEHVVPYGLGSPRS
(Disulfide bridge: 1-15 and 3-11)

0.5 mg

1 mg

62946-05

62946-1

Big Endothelin 1 (1-39), porcine
CSCSSLMDKECVYFCHLDIIWVNTPEHIVPYGLGSPSRS
(Disulfide bridge: 1-15 and 3-11)

0.25 mg

0.5 mg

1 mg

20713

20714

20715

Big Endothelin-1 (22-38), human
VNTPEHIVPYGLGSPSRS

1 mg

64858

Big Endothelin-1 (22-39), porcine
VNTPEHIVPYGLGSPSRS

1 mg

64859

Endothelin 1, human, porcine
CSCSSLMDKECVYFCHLDIIW
(Disulfide bridge:1-15 and 3-11)

0.25 mg

0.5 mg

1 mg

22859

22860

22861

Ac-[D-Trp16] Endothelin-1 (16-21), Receptor Antagonist Peptide 1, human
Ac-wLDIIW

1 mg

64864

[Ala1,3,11,16]-Endothelin 1, human
ASASSLMDKEAVYFAHLDIIW

0.5 mg

1 mg

24321

24322

Endothelin 2, human
CSCSSWLDKECVYFCHLDIIW
(Disulfide bridge:1-15 and 3-11)

0.25 mg

0.5 mg

1 mg

22862

22863

22864

Endothelin-2, mouse
CSCSNWLDKECVYFCHLDIIW
(Disulfide bridge:
1-15 and 3-11)

0.5 mg

62356

Endothelin 3, human, rat
CTCFTYKDKECVYYCHLDIIW
(Disulfide bridge:1-15 and 3-11)

0.5 mg

1 mg

24323

24324

[Tyr123] Prepro Endothelin (110 - 130), amide, human
CQCASQKDKKCWSYCQAGKEI-NH2
(Disulfide bridge:1-15 and 3-11)

0.5 mg

1 mg

64815-05

64815-1

BQ123, Cyclo(-wdPvL-), Endothelin Antagonist
Cyclo(-wdPvL-)

1 mg

62357

















































References
1 Palma, BD. et al. Brazilian J. Med. Biol. Res. 35, 75 (2002).
2 Lüscher, T. Circulation 102, 2434 (2000).
3 Fecteau, M. et al. Hypertension 46, 87 (2005).
4 Inoue, A. et al. J. Biol. Chem. 264, 14954 (1989).
5 Highsmith, RF. et al. FASEB J. 9, 1196 (1995).
6 Smith, K. et al. Br. J. Cancer 88, 163 (2003).
7 Boese, G. et al. J. Cardiovasc. Pharmacol. 36, S44 (2000).
8 Heilker, R. et al. Biochem. 43, 9021 (2004).
9 Higuchi, K. et al. J. Biol. Chem. 266, 18352 (1991).
10 Kobayashi, S. et al. J. Biol. Chem. 273, 12584 (1998).
11 Clark, JC. et al. Br. J. Pharmacol. 159, 812 (2010).