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Inhibitors
| Cat.No. | Name | Information |
|---|---|---|
| M13960 | Endothelin 1 (swine, human) (TFA) | Endothelin 1 (swine, human) (TFA) is a synthetic peptide with the sequence of human and swine Endothelin 1, which is a potent endogenous vasoconstrictor. Endothelin 1 acts through two types of receptors ETA and ETB. |
| M13959 | BQ-788 sodium salt | BQ-788 sodium salt is a potent and selective ETB receptor antagonist, inhibiting ET-1 binding to ETB receptors with an IC50 of 1.2 nM in human Girrardi heart cells. |
| M13958 | BQ-788 | BQ-788 is a potent, selective ETB receptor antagonist with IC50 of 1.2 nM for inhibition of ET-1 binding to human Girardi heart cells, poorly inhibiting the binding to ETA receptors in human neuroblastoma cell line SK-N-MC cells with IC50 of 1300 nM. |
| M13957 | Carperitide acetate | Carperitide acetate (Atrial Natriuretic Peptide (ANP) (1-28), human, porcine acetate) is a 28-amino acid hormone, that is normally produced and secreted by the human heart in response to cardiac injury and mechanical stretch. |
| M13956 | Aprocitentan | Aprocitentan (ACT-132577) is the major and pharmacologically active metabolite of Macitentan. Aprocitentan is dual ETA/ETB antagonist with IC50s of 3.4 nM and 987 nM, and pA2 valus of 6.7 and 5.5, respectively. |
| M10916 | RO 46-8443 | RO 46-8443 is the first non-peptide endothelin ETB receptor selective antagonist. RO 46-8443 displays up to 2000-fold selectivity for ETB receptors both in terms of binding inhibitory potency and functional inhibition. |
| M9792 | Sarafotoxin S6c | Sarafotoxin S6c is a highly selective ETB endothelin receptor agonist (Ki values are 0.29 and 28000 nM at ETB and ETA receptors respectively). |
| M9555 | Endothelin-1 (human, porcine) | Endothelin-1 (human, porcine) is a synthetic peptide with the sequence of human and swine Endothelin 1, which is a potent endogenous vasoconstrictor. |
| M9554 | BQ-123 | BQ-123 is a selective endothelin A receptors (ETAR) antagonist with an IC50 value of 7.3 nM. |
| M5135 | Ro-46-2005 | Ro 46-2005 is a novel synthetic non-peptide endothelin receptor antagonist, inhibits the specific binding of 125I-ET-1 to human vascular smooth muscle cells (ETA receptor) with IC50 of 220 nM. |
| M2467 | Bosentan | Bosentan is an endothelin (ET) receptor antagonist for ET-A and ET-B with Ki of 4.7 nM and 95 nM, respectively. |
| M2278 | Bosentan Hydrate | Bosentan is an endothelin (ET) receptors antagonist for ET-A and ET-B with Ki of 4.7 nM and 95 nM, respectively. |
| M2205 | Macitentan | Macitentan is an orally-active, tissue-targeting dual ET receptor antagonist. |
| M2029 | Sitaxsentan sodium | Sitaxsentan (TBC-11251) is an orally active, highly selective antagonist of endothelin A receptors. |
| M1951 | Ambrisentan | Ambrisentan is an orally active, highly selective antagonist of the endothelin-1 type A receptor. |
| M1816 | Zibotentan | Zibotentan (ZD4054) is a more selective and specific endothelin-A receptor (ETAR) antagonist with an IC50 value of 21 nM. |
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