endothelin 3

Endothelin-3 (human, mouse, rabbit, rat) is a cyclic 21-amino acid peptide, acting as an endogenous neuropeptide and potent vasoconstrictor.

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.

[Ala2] Endothelin-3, human 为ET-3的线性类似物，其结构中的Cys残基被Ala所替代。ET-3是由人体横纹肌肉瘤细胞系产生，且仅在此细胞系中表达的一种具有血管活性的肽。在非肌肉来源的肉瘤细胞系中不表达。该肽能够作为旁分泌因子，促进内皮细胞迁移。

[Ala1,3,11,15]-Endothelin (TFA) is a highly selective for endothelin A (ETA) and endothelin B (ETB) receptor.[Ala1,3,11,15]-Endothelin is a selective ETB endothelin receptor agonist (IC50 values are 0.33 and 2200 nM for displacing [125I]-ET-1 from ET

Selective ETB endothelin receptor agonist (IC50 values are 0.33 and 2200 nM for displacing [125I]-ET-1 from ETB and ETA receptors respectively).

[Ala1,3,11,15]-Endothelin (53-63) (TFA) 是一种ETB 激动剂。[Ala1,3,11,15]-Endothelin (53-63) (TFA) 对 ETB 具有选择性，IC50值范围为 0.33 nM 至 0.61 nM。[Ala1,3,11,15]-Endothelin (53-63) (TFA) 可用于血管收缩的研究。

GSK 2833503A is a potent and selective TRPC6 and TRPC3 antagonist (IC50 = 3-16 nM and 21-100 nM, respectively). GSK 2833503A exhibits >63-fold selectivity over other ion channels, including other TRP channels, CaV1.2, hERG and NaV1.5. GSK 2833503A suppresses angiotensin II or endothelin-1-induced cardiac hypertrophy signaling in HEK293 cellsin vitroand in cardiomyocytes.

Zibotentan (ZD4054) 是一种选择性的，具有口服活性的内皮素 A (ETA) 受体拮抗剂，Ki 为 13 nM。它具有抗癌作用，可研究去势抵抗性前列腺癌。

A-192621 is a potent, nonpeptide, orally active and selective endothelin B (ETB) receptor antagonist with an IC50 of 4.5 nM and a Ki of 8.8 nM. A-192621 promotes apoptosis in PASMCs and it also causes elevation of arterial blood pressure and an elevation

Atrial natriuretic peptide (3-28) (human) 是由心房心肌细胞合成并分泌的肽类激素，主要在调节血压、体液平衡及电解质稳态方面发挥作用。

Endothelin-1 is one of the there isoforms of endothelin (identified as ET-1, -2, -3) with varying regions of expression and binding to at least four known endothelin receptors, ETA, ETB1, ETB2 and ETC.

ACT-373898 is a metabolite of the endothelin (ET) receptor type A (ETA) and ETBdual antagonist macitentan .1 1.Dingemanse, J., Sidharta, P.N., Maddrey, W.C., et al.Efficacy, safety and clinical pharmacology of macitentan in comparison to other endothelin receptor antagonists in the treatment of pulmonary arterial hypertensionExpert Opin. Drug Saf.13(3)391-405(2013)

Zofenoprilat是一种血管紧张素转换酶(ACE; IC50 = 8 nM for the rabbit lung enzyme)的抑制剂，同时也是前体药zofenopril的活性代谢产物。它能够抑制分离的豚鼠小肠中由血管紧张素I或缓激肽诱导的收缩(EC50s = 3 and 1 nM, respectively)。在人类脐静脉内皮细胞(HUVECs)中，Zofenoprilat (10 nM)降低基础内皮素-1分泌和一氧化氮(NO)生成，并阻止TNF-α诱导的活性氧种(ROS)增加以及谷胱甘肽(GSH)水平降低。Zofenoprilat (10 µM)保护初级人类心脏微血管内皮细胞免受多柔比星诱导的细胞毒性。此外，Zofenoprilat (10 µM)还能增加HUVECs中的硫化氢(H2S)生成，以及细胞的黏着、迁移和增殖。在以400 µM浓度使用时，它可以减少Langendorff分离的大鼠心脏灌流缺血再灌注损伤模型中的舒张末压和乳酸脱氢酶(LDH)释放。

BQ-123 TFA 是一种高效、选择性内皮素 A(ETA)受体拮抗剂，IC50值为 7.3 nM，Ki 值为 25 nM。BQ-123 TFA 抑制内皮素-1 介导的人肺动脉平滑肌细胞增殖，降低高血压大鼠血压。

Sarafotoxin S6a TFA 是一种 Sarafotoxin 类似物，是一种内皮素受体 (endothelin receptor) 激动剂，具有与 Endothelin-3 相似的 ETA ETB 选择性。Sarafotoxin S6a TFA 诱导猪冠状动脉的 EC50值为 7.5 nM。