et-a

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]

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

Bosentan (Benzenesulfonamide) is a sulfonamide-derived, competitive and specific endothelin receptor antagonist with a slightly higher affinity for the endothelin A receptor than endothelin B receptor. Bosentan blocks the action of endothelin 1, an extremely potent endogenous vasoconstrictor and bronchoconstrictor, by binding to endothelin A and endothelin B receptors in the endothelium and vascular smooth muscle. Bosentan decreases both pulmonary and systemic vascular resistance and is particularly used in the treatment of pulmonary arterial hypertension.

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

Atrasentan hydrochloride (ABT-627 hydrochloride) is an endothelin receptor antagonist with an IC50 of 55.1 μM for ETA.

Atrasentan (ABT-627) is an endothelin receptor antagonist that can inhibit the activity of ETA (IC50 value is 0.0551 nM).

Aprocitentan (ACT-132577) is ETA and ETB antagonist .

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.

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.

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.

BQ-788 is a selective and potent ETB receptor antagonist with potential hypertensive activity.BQ-788 inhibits ET-1 binding to ETB receptors and inhibits exogenous ET-1-induced elevation of coronary artery perfusion pressure.

Aminaftone, a derivative of 4-aminobenzoic acid, inhibits endothelin-1 (ET-1) production and is used to study hypertension and systemic sclerosis.

Edonentan is A potent endothelin A (ETA) receptor antagonist that can be used to study heart failure.