Big Endothelin-1 (1-31) (human, bovine) trifluoroacetate salt

Endothelin-1 (1-31) (Human) is a potent vasoconstrictor and hypertensive agent. Endothelin-1 (1-31) (Human) is derived from the selective hydrolysis of big ET-1 by chymase[1].

Research Areas >> Cardiovascular Disease

Signaling Pathways >> MAPK/ERK Pathway >> ERK

Signaling Pathways >> Stem Cell/Wnt >> ERK

Endothelin-1 (1-31) (Human) (100 pM-100 nM; 24 h) 诱导人系膜细胞增殖[2]。 Endothelin-1 (1-31) (Human) (100 nM; 0-10 min) 在人系膜细胞中诱导 ERK 激活[2]。 Cell Proliferation Assay[2] Cell Line: Human mesangial cells Concentration: 100 pM-100 nM Incubation Time: 24 h Result: Caused an increase in [3H]-thymidine incorporation into the cells in a concentration-dependent manner. Western Blot Analysis[2] Cell Line: Human mesangial cells Concentration: 100 nM Incubation Time: 0, 5, 10, 15 and 30 min Result: ERK activities rapidly increased 2.45-fold at 5 min and peaked at 10 min. The activities of both ERKs rapidly declined, returning to the baseline control value 30 min after stimulation.

ET-1 (1-31) (100 nM; single dose) 诱导小鼠肠系膜动脉收缩。收缩可能是由 ETA 受体介导的，并可能随着年龄的增长而增加。在目前的慢性糖尿病的情况下，男性和女性之间存在明显差异[1]。 Animal Model: ICR mice, Streptozocin (HY-13753)-induced diabetic model[1] Dosage: 100 nM Administration: In the organ bath, single dose Result: In the 1-week control (but not diabetic) group, induced contraction and the contractile response was significantly greater in female mice than in male mice, and there was no significant difference in either male or female mice between the age-matched controls and the diabetic mice. In the 8-weeks group, the contraction was or tended to be increased compared with the corresponding 1-week group in all mice. Although in male mice this contraction was not different between control and diabetic groups, it was significantly greater in diabetic female mice than in the control female mice and in female diabetic mice than in male diabetic mice. The contraction was inhibited by ETA receptor inhibitor.

[1]. Matsumoto T, et al. Gender differences in vascular reactivity to endothelin-1 (1-31) in mesenteric arteries from diabetic mice. Peptides. 2008 Aug;29(8):1338-46.  

[2]. Yoshizumi M, et al. Effect of endothelin-1 (1-31) on human mesangial cell proliferation. Jpn J Pharmacol. 2000 Oct;84(2):146-55.