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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]

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.

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.

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

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

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.

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

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.

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

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

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.

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].

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).

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.

AMPA receptor modulator-2 (Example 134) is an AMPA receptor modulator with a pIC50 of 10.1 for TARPγ2 dependent AMPA receptor[1]. pIC50 = -lgIC50. [1]. BERRY CYNTHIA G B (US), et al. AZABENZIMIDAZOLES AND THEIR USE AS AMPA RECEPTOR MODULATORS. Patent. WO2016176460.

Et-29 is a selective inhibitor of SIRT5 inhibitor with a Ki of 40 nM.

SB-209670 is a selective endothelin receptor antagonist that inhibits the activity of ET(B) receptors in rat vascular endothelium and vascular smooth muscle.

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