Acetyl-(Ala11.15)-Endothelin-1 (6-21) ammonium salt

Names

[ Name ]:
Acetyl-(Ala11.15)-Endothelin-1 (6-21) ammonium salt

[Synonym ]:
N-Acetyl-[Ala11,15]-Endothelin 1 fragment 6-21
MFCD00214633
Acetyl-(Ala 11,15)-ET 1 (6-21)
N-Acetyl-L-leucyl-L-methionyl-L-α-aspartyl-L-lysyl-L-α-glutamyl-L-alanyl-L-valyl-L-tyrosyl-L-phenylalanyl-L-alanyl-L-histidyl-L-leucyl-L-α-aspartyl-L-isoleucyl-L-isoleucyl-L-tryptophan
L-Tryptophan, N-acetyl-L-leucyl-L-methionyl-L-α-aspartyl-L-lysyl-L-α-glutamyl-L-alanyl-L-valyl-L-tyrosyl-L-phenylalanyl-L-alanyl-L-histidyl-L-leucyl-L-α-aspartyl-L-isoleucyl-L-isoleucyl-

Biological Activity

[Description]:

BQ-3020 is a selective endothelin receptor (ETB receptor) agonist that displaces [125I] ET-1 binding to ETB receptors, with an IC50 value of 0.2 nM. BQ-3020 elicits vasoconstriction in the rabbit pulmonary artery. BQ-3020 makes relaxation of the pig urinary bladder neck and can be used for cardiovascular disease research12.

[Related Catalog]:

Research Areas >> Cardiovascular Disease

Signaling Pathways >> GPCR/G Protein >> Endothelin Receptor

[Target]

ETB:0.2 nM (IC50)

[References]

[1]. Arteaga JL,et.al. Endothelin ET(B) receptors are involved in the relaxation to the pig urinary bladder neck. Neurourol Urodyn. 2012 Jun;31(5):688-94.

[2]. Ihara M, et.al. A novel radioligand [125I]BQ-3020 selective for endothelin (ETB) receptors. Life Sci. 1992;51(6):PL47-52.

[3]. Quang PN, et.al. Peripheral endothelin B receptor agonist-induced antinociception involves endogenous opioids in mice. Pain. 2010 May;149(2):254-262.

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
2125.8±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C₉₆H₁₄₀N₂₀O₂₅S

[ Molecular Weight ]:
2006.32

[ Flash Point ]:
1239.5±34.3 °C

[ Exact Mass ]:
2005.001953

[ PSA ]:
730.82000

[ LogP ]:
6.02

[ Vapour Pressure ]:
0.0±0.3 mmHg at 25°C

[ Index of Refraction ]:
1.582

Safety Information

[ RIDADR ]:
NONH for all modes of transport

Articles

Endothelin-1 stimulates aldosterone synthesis in Conn's adenomas via both A and B receptors coupled with the protein kinase C- and cyclooxygenase-dependent signaling pathways.

J. Investig. Med. 48(5) , 343-50, (2000)

The mechanisms and factors leading to enhanced aldosterone secretion and ultimately to neoplastic transformation of the adrenal cortex are poorly defined. Angiotensin-II (Ang-II) and endothelin-1 (ET-...

Marked reduction of mortality in salt-loaded Dahl salt-sensitive rats by the new, selective endothelin ETA receptor antagonist, J-105859.

J. Hypertens. 18(12) , 1815-23, (2000)

To examine the chronic effects of a newly synthesized, potent and selective endothelin (ET) ETA receptor antagonist, J-1 05859, on mortality in salt-loaded Dahl salt-sensitive (DS) rats and to confirm...

Mechanisms involved in the effects of endothelin-1 in pig prostatic small arteries.

Eur. J. Pharmacol. 640(1-3) , 190-6, (2010)

Since endothelin-1 (ET-1) is involved in prostatic disorders, the current study investigated the mechanisms underlying the ET-1-induced effects in pig prostatic small arteries. The experiments were pe...