66 products were found matching "K04197"!

In mammals, the endothelin (ET) family comprises three endogenous isoforms: ET-1, ET-2, and ET-3. These endothelium-derived peptides perform their functions via two endothelin receptors, classified as EDNRA and EDNRB. EDNRA receptors are mainly localized in the vascular smooth muscle cells, where they are the...

Description: Ambrisentan (BSF 208075) is an endothelin receptor antagonist used in the therapy of pulmonary arterial hypertension (PAH). Ambrisentan has been associated with a low rate of serum enzyme elevations during therapy but has yet to be implicated in cases of clinically apparent acute liver injury. Target:...

Potent and selective endothelin receptor A (ETA) antagonist, suppresses the ET-1-induced decrease of LPL activity, shows protective effects in ischemic acute renal failure, neuroprotective, anti-hypertensive, inhibits ET-1 receptor binding and blocks Ca2 mobilization, cellular contraction and MAP kinase activation,...

Macitentan is a dual antagonist of the endothelin (ET) receptors type A and B (IC50s = 0.5 and 391 nM in a radioligand binding assay using recombinant ETA and ETB, respectively). Macitentan inhibits intracellular Ca2+ increases induced by the endothelin isoform ET-1 in human pulmonary arterial smooth muscle cells...

Ambrisentan is a nonpeptide endothelin A (ETA) receptor antagonist (IC50s = 0.251, 0.316, 0.398, 251, and 630 nM for rat preparations of heart, bladder, kidney, lung, and cerebral cortex, respectively). It inhibits contraction of isolated rabbit aortic rings induced by endothelin-1 (ET-1, Cay-24127) by 43.23% when...

Sitaxentan is a potent nonpeptide endothelin A (ETA) receptor antagonist (IC50 = 1.4 nM). It is selective for ETA over ETB receptors (IC50 = 9,800 nM). Sitaxentan inhibits phosphoinositol hydrolysis induced by endothelin-1 (Cay-24127) in COS-7 cells (pA2 = 8). In vivo, sitaxentan reduces blood pressure in a rat...

Bosentan-d4 is an internal standard for the quantification of bosentan (Cay-11731) by GC- or LC-MS. Bosentan is an antagonist of the endothelin receptors type A (Ki = 6.5 nM) and type B (Ki = 340 nM).Formal Name:...

Antibiotic, Potent endothelin receptor antagonist, Anti-osteoporotic, Antibacterial, Cytotoxic, Mediates its cytotoxic effects, at least in part, through proteasome inhibition. Isolated from Streptomyces violaceoruber.

Zibotentan is a selective antagonist of the endothelin (ET) receptor type A (IC50s = 21 and >10,000 nM for human recombinant ETA and ETB, respectively). It inhibits growth of HEY, OVCA 433, SKOV3, and A2780 cells induced by endothelin 1 (ET-1, Cay-24127) in vitro. Zibotentan reduces ET-1-induced expression of MMP-2,...

Macrolide, ET antagonist, proteasome inhibitor.

Macitentan is a dual endothelin receptor (ET-A/B)antagonist that displays antihypertensive, anti-fibrotic, and anticancer activity, this compound exhibits slower receptor dissociation kinetics than other endothelin receptor antagonists. Macitentan is currently used to treat pulmonary arterial hypertension, as...