endothelin-1 (et-1)

Aminaftone 是 4-氨基苯甲酸的衍生物，可抑制内皮素-1 (ET-1) 的产生，可用于研究高血压和系统硬化症。

Clazosentan (Ro 61-1790) 是一种特异性内皮素 A (ETA）受体拮抗剂,抑制 ET-1 介导的血管痉挛。Clazosentan 可用于研究神经系统疾病和心血管疾病。

Bosentan (Benzenesulfonamide) 是 endothelin-1 (ET)拮抗剂，在人的 SMC 细胞中，它能够作用于 ETA 受体(Ki:4.7 nM)和 ETB 受体(Ki:95 nM)。

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

ENDOTHELIN-1 (ET-1), the principal peptide of the endothelin family, has been shown to have a variety of biological activities in both vascular and nonvascular tissues. The C-terminal fragment, which is a highly conserved sequence in the peptides of t

Ac-Endothelin-1 (16-21), human acetate 是内皮素家族的主要肽，已被证明在血管和非血管组织中具有多种生物活性。 C-末端片段是 ET 家族肽中高度保守的序列，已显示可区分称为 ETA 和 ETB 的两种 ET 受体亚型，因为它仅激活后者。

J-104132 is a potetn and selective endothelin A B receptor antagonist (Ki: cloned human ETA = 0.034 nM; cloned human ETB = 0.104 nM) . In vitro, J-104132 is a potent antagonist of ET-1-induced accumulation of [3H]inositol phosphates in Chinese hamster ova

Ro 46-2005是新型非肽类内皮素拮抗剂，能够抑制人血管平滑肌细胞(ETA 受体)(IC50:220 nM)。

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)

Nebentan (YM598) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist through the modification of Bosentan . Nebentan inhibits [125I] endothelin-1 binding to cloned human endothelin ETA and ETB receptor, with Ki of 0.697 nM and 569 nM, respectively[1]. YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo[2]. Nebentan inhibits the specific binding of [125I] endothelin-1 to endothelin ETA and ETB receptors in a concentration dependent manner,Ki values are 0.697 nM and 1.53 nM for human and rat endothelin ETA receptors, respectively. In contrast, YM598 exhibits low affinities for human and rat endothelin ETB receptors, with Ki values of 569 nM and 155 nM,respectively[1].In measurement of intracellular Ca2+ concentration, Nebentan concentration-dependently inhibits the increase in [Ca2+]i induced by 10 nM endothelin-1 in both CHO cells and A10 cells, the IC50 values are 26.2 nM for CHO cells and 26.7 nM for A10 cells, respectively[1]. Nebentan (oral administration; 0.1-1 mg kg; 4 weeks) significantly inhibits the progression of pulmonary hypertension and the development of right ventricular hypertrophy[2].Nebentan (oral administration; 1 mg kg; 30 weeks) significantly ameliorates the poor survival rate of CHF rats, it markedly reduces the hypertrophy of both ventricles as well as pulmonary congestion[2]. [1]. Hironori Yuyama, et al. Pharmacological Characterization of YM598, an Orally Active and Highly Potent Selective Endothelin ET(A) Receptor Antagonist. Eur J Pharmacol. 2003 Sep 30;478(1):61-71. [2]. Akira Fujimori, et al. YM598, an Orally Active ET(A) Receptor Antagonist, Ameliorates the Progression of Cardiopulmonary Changes and Both-Side Heart Failure in Rats With Cor Pulmonale and Myocardial Infarction. J Cardiovasc Pharmacol. 2004 Nov;44 Suppl 1:S354-7.

Human Big ET-1 comprises residues 53-90 of the endothelin precursor (preproendothelin). Compared to the mature endothelin-1 (hET-1), the peptide show less vasoconstrictor activity in vitro, but similar pressor effects in vivo. Former CAS-number 121014-53-7.

The big endothelins comprise residues 53-90 (human big ET-1) and 53-91 (porcine big ET-1) of the endothelin precursor (preproendothelin). Compared to the mature endothelin-1 (ET-1), both peptides show less vasoconstrictor activity in vitro, but similar pressor effects in vivo. Former CAS-number 121014-54-8.

Thrombin receptor agonist peptide (TRAP-14) is a 14-amino acid peptide agonist of the α-thrombin receptor. It induces aggregation of washed platelets as well as platelets in citrated and hirudin plasma. TRAP-14 (100 μM) increases the cytosolic calcium concentration in isolated guinea pig pulmonary smooth muscle cells 5-fold over baseline. It increases pulmonary arterial pressure in isolated guinea pig lung when used at a concentration of 1 μM, which is comparable to the effect induced by 10 nM α-thrombin. TRAP-14 also induces contraction of isolated rat aortic rings and increases endothelin-1 (ET-1) levels in a dose-dependent manner, an effect that is reversed by the ETA antagonist BQ-123 and the nitric oxide synthase (NOS) inhibitor L-NNA .

Desmethyl bosentan is an active metabolite of the endothelin receptor antagonist bosentan .1Desmethyl bosentan (25 μM) activates the pregnane X receptor (PXR) in CV-1 monkey kidney cells expressing the human receptor in a reporter assay. 1.van Giersbergen, P.L.M., Gnerre, C., Treiber, A., et al.Bosentan, a dual endothelin receptor antagonist, activates the pregnane X nuclear receptorBr. J. Clin. Pharmacol.54(5)561-562(2002)

BE-24566B is a polyketide fungal metabolite originally isolated fromS. violaceusniger.1It is active againstB. subtilis,B. cereus,S. aureus,M. luteus,E. faecalis, andS. thermophilus(MICs = 1.56, 1.56, 1.56, 1.56, 3.13, and 3.13 μg/ml, respectively). BE-24566B is an endothelin (ET) receptor antagonist (IC50s = 11 and 3.9 μM for ETAand ETBreceptors, respectively).2 1.Kojiri, K., Nakajima, S., Fuse, A., et al.BE-24566B, a new antibiotic produced by Streptomyces violaceusnigerJ. Antibiot. (Tokyo)48(12)1506-1508(1995) 2.Lam, Y.K.T., Hensens, O., Helms, G., et al.L-755,805, a new polyketide endothelin binding inhibitor from an actinomyceteTetrahedron Lett.36(12)2013-2016(1995)

Bosentan hydrate (Ro 47-0203) 是endothelin-1 (ET)竞争性拮抗剂，在人SMC 细胞中，它能够作用于 ETA 受体(Ki:4.7 nM)和 ETB 受体(Ki:95 nM)。

Bosentan-d4 是 Bosentan 的氘代物。Bosentan 是一种有效的endothelin-1 (ET)拮抗剂，在人的 SMC 细胞中，作用于ETA 和ETB 受体，Ki 值分别为 4.7 nM 和 95 nM。

Endothelin 1 (swine, human) (TFA) 是具有人和猪内皮素 1 序列的合成肽，是有效的内源性血管收缩剂。Endothelin 1 通过两种类型受体 ETA 和 ETB 发挥作用。

Endothelin 1 (swine, human), Alexa Fluor 488-labeled 是标记了488 荧光的 Endothelin 1 合成肽。Endothelin 1 (swine, human) 是具有人和猪内皮素 1 序列的合成肽，是有效的内源性血管收缩剂。Endothelin 1 通过两种类型受体 ETA 和 ETB 发挥作用。

[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。

Endothelin-1 (1-31) (Human) 是源于chymase对大ET-1选择性水解而来的有效血管收缩剂和血压升高剂。

Endothelin-1 (1-31) (Human) acetate，源自于chymase对大ET-1的选择性水解，是一种有效的血管收缩剂和血压升高剂。

Endothelin-1 (1-31) (Human) TFA 是源自chymase对大ET-1选择性水解的一种有效血管收缩剂和血压升高剂。

BQ-3020 ammonium 是一种内皮素受体（endothelin receptor）(ETB receptor) 激动剂。它在阻断[125I]ET-1与猪小脑ETB受体的结合实验中显示出IC50值为0.2 nM。此外，BQ-3020 ammonium能够引致兔肺动脉血管收缩以及猪膀胱颈的松弛，因此可作为心血管疾病研究的工具。