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Endothelin Receptor Endothelin Receptor

Inhibitors

Cat.No.  Name Information
M20689 Sparsentan (PS-433540,RE-021,DARA) Sparsentan (PS-433540, RE-021, DARA) is A dual antagonist of the endothelin type A receptor(ETA) and Angiotensin II type 1 receptor.
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 an effective and selective ETB receptor antagonist with an IC50 of 1.2 nM in human Girrardi heart cells to inhibit ET-1 binding to the ETB receptor. BQ-788 is an enhancer of AQP4(Aquaporin-4).
M13958 BQ-788 BQ-788 is a potent and selective ETB receptor antagonist with an IC50 of 1.2 nM inhibiting ET-1 binding to ETB receptor in human Girrardi heart cells. BQ-788 is an enhancer of AQP4(Aquaporin-4).
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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