Endothelin Receptor (inhibitors, antagonists, agonists)-ProbeChem.com

Request The Product List ofEndothelin Receptor Endothelin Receptor

Cat. No.	Product Name	Information
PC-60030	Aprocitentan Endothelin receptor antagonist	Aprocitentan (ACT132577) is the major and pharmacologically active metabolite of Macitentan, an orally active, dual endothelin receptor antagonist with IC50s of 3.4 nM and 987 nM for ETA/ETB receptor respectively, inhibits ET-1 and ET-2-induced contractions in functional assays.
PC-45639	Ro 46-2005 Endothelin receptor antagonist	Ro 46-2005 is the first synthetic orally active nonpeptide antagonist of endothelin receptor with equipotent potency (IC50=0.2-0.5 uM) for ETA and ETB.
PC-42282	Zibotentan ETA receptor inhibitor	Zibotentan (ZD4054) is an orally active, specific Endothelin A receptor (ETA) inhibitor with Ki of 13 nM, shows anticancer effects.
PC-45971	Sitaxsentan ETA receptor inhibitor	Sitaxsentan (IPI-1040, Sitaxentan) is a potent, long acting, orally active, selective ETA receptor antagonist that binds competitively to human ETA receptor with Ki of 0.43 nM, IC50 of 1.4 nM.
PC-42811	Sitaxsentan sodium ETA receptor inhibitor	Sitaxsentan sodium (TBC11251, IPI 1040) is a potent, long acting, orally active, selective ETA receptor antagonist that binds competitively to human ETA receptor with Ki of 0.43 nM, IC50 of 1.4 nM.
PC-28489	Nebentan ETA antagonist	Nebentan (Nebentan potassium, YM598) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist, inhibits [125I] endothelin-1 binding to cloned human ETA receptor with Ki of 0.697 nM, >800-fold selective over ETB receoptor.
PC-26608	PD-156707 ETA receptor antagonist	PD-156707 is a potent, selective and orally active non-peptide endothelin-A (ETA) receptor antagonist with Ki of 0.17 nM, >500-fold selective over ET-B receptor.
PC-25045	Darusentan ETA receptor antagonist	Darusentan (Lu-135252) is a selective endothelin receptor A (ETA) receptor antagonist with binding Ki of 1.4 nM, >100-fold selective over ET-B receptor.
PC-25044	Macitentan Endothelin receptor antagonist	Macitentan (ACT-064992) is a potent, selective and orally active dual ETA/ETB endothelin receptor antagonist with binding IC50 of 0.5/391 nM for ETA/ETB receptors respectively.
PC-25043	Pipersentan ETA receptor antagonist	Pipersentan (Diosuxentan) is a potent, selective endothelin receptor A (ETA receptor) antagonist, inhibits binding of 125I-ET-1 toward recombinant ETA receptor with IC50 of 4.44 nM, >1000-fold selective over ETB receptor.
PC-24438	RES-701-3 ETB receptor antagonist	RES-701-3 is a potent, selective antagonist of endothelin type B receptor (ETB receptor) with IC50 of 31.5 nM, with no activity against ETA. RES-701-3 functions as an inverse agonist.
PC-23821	BQ-788 sodium salt ETB receptor antagonist	BQ-788 sodium salt is a potent, selective endothelin-B receptor (ETB) antagonist with IC50 of 1.2 nM for inhibition of ET-1 binding to human Girardi heart cells, >1000-fold selective over ETA receptor.

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