et-rb

Endothelin-2 (49-69), human (Human endothelin-2) 是一种由 21 个氨基酸组成的血管活性肽。它可与 G 蛋白连接的跨膜受体，ET-RA 和ET-RB 结合。

N-(6-chloro-5-(2-Methoxyphenoxy)-2-(pyridin-4-yl)pyriMidin-4-yl)-5-Met 抑制内皮素与CHO 细胞膜上人ETA 受体和人ETB 受体的的结合,IC50分别为268nM 和 1810nM。

Endothelin-2 (49-69), human (TFA) is a 21-amino acid vasoactive peptide that binds to ET-RA and ET-RB.

TREK1 and TREK2 channel activator (EC50 = 0.76 μM in Rb efflux assay in TREK1-expressing CHO cells). Exhibits selectivity for TREK1/2 over TRAAK, TASK3 and a range of other potassium channels. Hyperpolarizes membrane potential of dorsal root ganglion neurons and depresses neuronal activity in vitro. Loucif et al (2018) GI-530159, a novel, selective, mechanosensitive two-pore-domain potassium (K2P) channel opener, reduces rat dorsal root ganglion neuron excitability. Br.J.Pharmacol. 175 2272 PMID:29150838

Endothelin-3, human, mouse, rabbit, rat TFA is a 21-amino acid vasoactive peptide that specifically interacts with G-protein-linked transmembrane receptors, ET-RA and ET-RB.