eta and etb

Endothelin 1 (swine, human), a synthetic peptide mirroring the sequence of both human and swine Endothelin 1, functions as a robust endogenous vasoconstrictor by interacting with two receptor types, ETA and ETB.

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。

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)。

Aprocitentan D4 (ACT-132577 D4) is a deuterium-labeled Aprocitentan. Aprocitentan is a major and pharmacologically active metabolite of Macitentan. Aprocitentan is a dual ETA ETB antagonist (IC50s: 3.4 nM and 987 nM; pA2s: 6.7 and 5.5).

Macitentan-d4 (ACT-064992 D4) 是一种 Macitentan 氘代物，可被当作非多肽 ETA 和 ETB  (内皮素受体)双拮抗剂。Macitentan-d4 比 Macitentan 毒性更低，半衰期更长，可用于研究由内皮素受体介导介导的疾病。

Macitentan n-butyl analogue, a derivative of Macitentan, functions as an orally active dual antagonist targeting both endothelin ETA and ETB receptors. This compound shows promise for treating idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH), leveraging its non-peptide structure for potential therapeutic applications.

PD-159020 is a non-selective antagonist of ETA ETB(hETA and hETB with IC50s of 30 and 50 nM , respectively).

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

IRL-1620 acetate 是一种有效的特异性内啡肽 B 受体 (ETB) 激动剂，Ki 为 16 pM，相比于ETA，其Ki 为 19 μM。

Tezosentan is an antagonist of the endothelin receptor (pA2s: 9.5, 7.7 for ETA and ETB receptors, respectively).

Endothelin 1 (swine, human) acetate(117399-94-7 free base) 是一种合成肽，其序列为人和猪内皮素 1。它是一种有效的内源性血管收缩剂，通过两种类型的受体 ETA 和 ETB 起作用。

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 46-844 是选择性非肽内皮素受体拮抗剂。它对ETB(IC50: 34-69 nM) 的选择性比ETA 受体 (IC50: 6800 nM) 高的100倍以上。

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.

Sclerotiorin is a natural product isolated primarily from Penicillium species. It inhibits soybean lipoxygenase-1 with an IC50 value of 4.2 μM. Sclerotiorin also exhibits a number of other activities including inhibition of cholesterol ester transfer protein (IC50 = 19.4 μM),, inhibition of Grb2-Shc interaction (IC50 = 22 μM),, and antagonism of endothelin receptors (IC50 = 114 and 152 μM for human ETA and ETB, respectively).

Darusentan (Lu-135252) 是内皮素受体 A (ET-A) 受体选择性拮抗剂，能够作用于 ET-A 受体(Ki:1.4 nM)及ET-B 受体(Ki:184 nM)，对 ETA 受体的选择性大于 ETB 受体的100以上。它在大鼠主动脉血管平滑肌细胞膜中竞争结合放射性标记的内皮素(Ki:13 nM)。

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。

Aprocitentan (ACT-132577) 是一种 Macitentan 的主要活性代谢物。它是 ETA ETB 的双重拮抗剂，其 pA2值分别为 6.7 和 5.5，IC50分别为 3.4 nM 和 987 nM。

N-Despropyl Macitentan-d4 是 N-Despropyl Macitentan 的氘代化合物。N-Despropyl Macitentan 的 CAS 号为 1103522-45-7。Aprocitentan 是一种 Macitentan 的主要活性代谢物。它是ETA ETB的双重拮抗剂，其pA2值分别为 6.7 和 5.5，IC50分别为 3.4 nM 和 987 nM。