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Macitentan (ACT-064992) is an endothelin receptor antagonist utilized in the treatment of pulmonary arterial hypertension (PAH).

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 elevates both arterial blood pressure and plasma ET-1 levels[1][2][3]. Its selectivity is 636-fold higher for ETB than ETA (IC50 of 4280 nM and Ki of 5600 nM).

Zibotentan (ZD4054) (ZD4054) is a specific Endothelin (ET)A antagonist with IC50 of 21 nM, exhibiting no activity at ETB. Phase 3.

IRL 2500 is an antagonist of Endothelin receptor with IC50s of 1.3 and 94 nM for Endothelin A receptor and Endothelin B receptor.

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

Macitentan-d4 (ACT-064992 D4) is a deuterated substitute for Macitentan and can be used as a dual antagonist of the non-peptides ETA and ETB (endothelin receptor).Macitentan-d4 is less toxic than Macitentan, has a longer half-life, and can be used to study endothelin receptor-mediated diseases.

ETA antagonist 1 is an antagonist of ETA selective (IC50 of 0.08 μM).

Endothelin 1 (swine, human) is a potent endogenous vasoconstrictor peptide released primarily by endothelial cells and acting through ETA and ETB receptors. Endothelin 1 (swine, human) mediates vascular smooth-muscle contraction, promotes fibrosis, stimulates reactive oxygen species production, and induces pro-inflammatory signaling, making it central to studies of vascular dysfunction, hypertension, and oxidative stress–associated pathology.

Phe-Met-Arg-Phe Like Peptide acetate (Pqdpflrfamide acetate) is a FMRF-like peptide from visceral and somatic muscles of the snail Helix aspersa. FMRF (Phe-Met-Arg-Phe) is a neuropeptide peptide consisting of 4 amino acid residues.

Abz-Ala-Pro-Glu-Glu-Ile-Met-Arg-Arg-Gln-EDDnp is a fluorescence-quenched peptide substrate for human neutrophil elastase (kcat/Km = 531 mM-1s-1). Enzymatic peptide hydrolysis disrupts the Abz:EDDnp donor-acceptor pair allowing fluorescence measurement of Abz (ex = 320 nm; em = 420 nm).

H-Leu-Trp-Met-Arg-OH, a tetrapeptide, serves as a substrate for studies on aminopeptidase-mediated hydrolysis [1].

Met-Arg-Phe-Ala, a peptide, serves as a potent competitive inhibitor of enkephalin-generating endopeptidase (EGE) and is utilized in neurological disease research [1].

Phe-Met-Arg-Phe-like peptide, derived from the visceral and somatic muscles of the snail Helix aspersa, is a neuropeptide known as FMRF (Phe-Met-Arg-Phe). This peptide comprises four amino acid residues[1].

Phe-met-arg-phe amide trifluoroacetate is an activator of K+ current with an ED50 of 23nm on the fundus nerve.

N-Formyl-Met-Ala-Ser is a peptide that binds to formyl peptide receptors on neutrophils. N-Formylmethionine-containing peptides, including the most potent and well-known member N-formyl-Met-Leu-Phe [FMLP or fMet-Leu-Phe], stimulate human neutrophils through a receptor-dependent mechanism.

N-Formyl-Met-Ala-Ser TFA (17351-32-5 free base) is a peptide that binds to formyl peptide receptors on neutrophils. This N-formylmethionine-containing peptide, called fMet-Ala-Ser, is one of the most potent and best-known peptides that interact with these receptors.

Phe-Met-Arg-Phe, amide dose-dependently (ED50=23 nM) activates a K+ current in peptidergic caudodorsal neurons and appears to localize with neuropeptide Y in some brain regions.

Phe-Met-Arg-Phe, amide acetate, activates a K+ current in peptidergic caudodorsal neurons dose-dependently (ED50=23 nM) and appears to localize with neuropeptide Y in some brain regions.

Met-AMS TEA (compound 50) is an aminosulfonate analog of methionyl adenosylsulfate, effectively inhibiting Escherichia coli methionyl-tRNA synthetase (MetRS) with an IC50 of 7 nM.

Enrasentan (sb-217242) is a mixed antagonist of ET(A) and ET(B) receptors that reduces blood pressure, prevents cardiac hypertrophy, and protects myocardial function.

Nebentan potassium (YM598) is an orally active and selective nonpeptide endothelin receptor (ETA receptor) antagonist.Nebentan potassium inhibits pulmonary arterial hypertension and may be useful in the study of neurologic and cardiovascular diseases.

Clazosentan (Ro 61-1790) is a selective antagonist of the endothelin A receptor (ETAreceptor) that inhibits ET-1-mediated vasoconstriction, preventing cerebral vasospasm and vasospasm-associated cerebral infarction.

Avosentan(Ro 67-0565; SPP-301) is a potent endothelin receptor (ETA) antagonist with strong inhibitory effects on endothelin-1-induced contraction and may have protective effects against chronic kidney disease. [2]

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.