Endothelin-2 (human) (trifluoroacetate salt)

Endothelin-2 is a peptide vasoconstrictor and ligand for the endothelin (ET) receptors ETA and ETB (Kbs= 32.8 and 1.33 nM, respectively).1 It induces β-arrestin recruitment in CHO-K1 cells expressing human ETA and ETB (pD2s =8.75 and 8.55, respectively). Ex vivo, endothelin-2 induces vformal asoconstriction in isolated rat mesenteric arterial beds (ED50 = 90.8 pmol).2 Endothelin-2 also induces contraction of isolated rat uteri, an effect which is reversed by the ETA antagonist BQ-123 but not the ETB antagonist BQ-788 (Item No. 17403).3 Infusion of endothelin-2 restores vasoconstriction of vessels at the follicular apex of the ovarian follicle and ovulation in Amhr2cre/+Smo2 mice.4WARNING This product is not for human or veterinary use.

[1] JANET J. MAGUIRE . Comparison of human ETA and ETB receptor signalling via G-protein and β-arrestin pathways[J]. Life sciences, 2012, 91 13: Pages 544-549. DOI: 10.1016/j.lfs.2012.03.021
[2] STEPHEN A. DOUGLAS  C. R H. Endothelium-dependent vascular activities of endothelin-like peptides in the isolated superior mesenteric arterial bed of the rat[J]. British Journal of Pharmacology, 1990, 101 1: 81-88. DOI: 10.1111/j.1476-5381.1990.tb12093.x
[3] MARIA KOUSIDES  Jocelyn N P  Margot E Story. Endopeptidase 24.11 inhibition does not modify uterotonic effects of endothelins in rat uterus[J]. Peptides, 1998, 19 9: Pages 1585-1593. DOI: 10.1016/s0196-9781(98)00105-3
[4] FERNANDO F MIGONE. In vivo imaging reveals an essential role of vasoconstriction in rupture of the ovarian follicle at ovulation.[J]. Utilitas, 2016, 4 1: 2294-2299. DOI: 10.1073/pnas.1512304113