CAS#:123562-20-9 | Endothelin-2 (human, canine) acetate salt

[Description]:

Endothelin-2, human 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 >> Others

Research Areas >> Cardiovascular Disease

Peptides

[Target]

ET-RA, ET-RB[1]

[In Vitro]

At nanomolar concentrations, Endothelin-2 exhibits a strong and long-lasting vasoconstrictor activity characteristic of endothelin (EC50=0.52 nM)[1]. Endothelin-2 is a chemoattractant for macrophages and THP-1 monocytic cells, but not for freshly isolated monocytes. The chemotactic response to Endothelin-2 shows a typical bell-shaped response curve. Experiments with endothelin receptor antagonists shows that migration to Endothelin-2 is mediated via the ET-RB receptor. Endothelin-2 expression by tumors may modulate the behavior of macrophages such that activated cells accumulate in areas of hypoxia[2].

[In Vivo]

Two distinct phases of pressor effects are typically seen in response to Endothelin-2: the early phase immediately follows the depressor response and dominates during the next 3-10 min, whereas the late pressor effect develops 10-20 min after the injection and lasts >1 hr[1].

[Animal admin]

Rats[1] For the assay of pressor activity, male Wistar rats weighing 300-350 g are anesthetized with urethane (1 g/kg i.p.) and pretreated with atropine (0.25 mg/kg i.v.), propranolol (1 mg/kg i.v.), and bunazocine (1 mg/kg i.v.). Additional maintenance doses (one-half of the initial doses) of the autonomic blockades are administered every 3-4 hr. Each animal is given only one bolus of Endothelin-2. 1 nM of Endothelin-2 in 50 μL of buffer is bolus injected from a cannula inserted in the right femoral vein. The blood pressure is recorded from a cannula, which is placed in the right carotid artery and connected to a pressure transducer[1].

[References]

[1]. Grimshaw MJ, et al. Endothelin-2 is a macrophage chemoattractant: implications for macrophage distribution in tumors. Eur J Immunol. 2002 Sep;32(9):2393-400.

[Related Small Molecules]

[ Molecular Formula ]:
C₁₁₅H₁₆₀N₂₆O₃₂S₄

[ Molecular Weight ]:
2546.92000

[ Exact Mass ]:
2545.06000

[ PSA ]:
1025.62000

[ LogP ]:
4.59880

[ Appearance of Characters ]:
powder | white

[ Storage condition ]:
−20°C

Click to get detail MSDS

[ Symbol ]:

GHS06

[ Signal Word ]:
Danger

[ Hazard Statements ]:
H300 + H310 + H330

[ Precautionary Statements ]:
P260-P264-P280-P284-P301 + P310-P302 + P350

[ Personal Protective Equipment ]:
Eyeshields;Faceshields;Gloves;type P2 (EN 143) respirator cartridges

[ Hazard Codes ]:
T+

[ Risk Phrases ]:
R26/27/28

[ Safety Phrases ]:
S28-S45-S36-S37

[ RIDADR ]:
UN 2811 6.1/PG 1

[ WGK Germany ]:
3

Role of the endothelin axis in astrocyte- and endothelial cell-mediated chemoprotection of cancer cells.

Neuro. Oncol. 16(12) , 1585-98, (2014)

Recent evidence suggests that astrocytes protect cancer cells from chemotherapy by stimulating upregulation of anti-apoptotic genes in those cells. We investigated the possibility that activation of t...

Cardiovascular changes in atherosclerotic ApoE-deficient mice exposed to Co60 (γ) radiation.

PLoS ONE 8 , e65486, (2013)

There is evidence for a role of ionizing radiation in cardiovascular diseases. The goal of this work was to identify changes in oxidative and nitrative stress pathways and the status of the endothelin...

The human endothelin family: three structurally and pharmacologically distinct isopeptides predicted by three separate genes.

Proc. Natl. Acad. Sci. U. S. A. 86 , 2863-2867, (1989)

Three distinct human endothelin-related genes were cloned by screening a genomic DNA library under a low hybridization stringency with a synthetic oligonucleotide probe encoding a portion of the endot...

Endothelin-2 (human, canine) acetate salt

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Chemical & Physical Properties

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Related Compounds