Endothelin Receptor Agonist

IRL-1620 is a potent and selective endothelin receptor type B (ETB) agonist with a K_i of 16 pM.

C-Type Natriuretic Peptide (CNP) (1-22), human (TFA),a 1-22 fragment of CNP, is a natriuretic peptide receptor B (NPR-B) agonist. C-Type Natriuretic Peptide (CNP) (1-22), human (TFA) inhibits cAMP synthesis stimulated by the physiological agonists histamine and 5-HT or directly by Forskolin. CNP is a potent, endothelial-derived relaxant and growthinhibitory factor.

IRL-1620 (TFA) is a potent and selective endothelin receptor type B (ETB) agonist with a K_i of 16 pM.

Sarafotoxin S6a, a sarafotoxin analogue, is a endothelin receptor agonist and has an ET_A/ET_B selectivity profile similar to that of Endothelin-3 (HY-P0204). Sarafotoxin S6a elicits the pig coronary artery with an EC₅₀ value of 7.5 nM.

Sarafotoxin S6c (SRTX-c) is a potent endothelin-B receptor agonist. Sarafotoxin S6c can cause vasoconstriction in both endothelium-intact and endothelium-denuded vessels.

BQ-3020 ammonium is a selective endothelin receptor (ET_B receptor) agonist. BQ-3020 ammonium inhibits [¹²⁵I] ET-1 binding to ET_B receptors, with an IC₅₀ value of 0.2 nM. BQ-3020 ammonium elicits vasoconstriction in the rabbit pulmonary artery. BQ-3020 ammonium makes relaxation of the pig urinary bladder neck and can be used for cardiovascular disease research. .

[Ala1,3,11,15]-Endothelin (53-63) (TFA) is an ET_B agonist. [Ala1,3,11,15]-Endothelin (53-63) (TFA) has selectivity for ET^B with IC₅₀ values range from 0.33 nM to 0.61 nM. [Ala1,3,11,15]-Endothelin (53-63) (TFA) can be used for the research of vasoconstriction.

[Ala1,3,11,15]-Endothelin (53-63) is an ET_B agonist. [Ala1,3,11,15]-Endothelin (53-63) has selectivity for ET^B with IC₅₀ values range from 0.33 nM to 0.61 nM. [Ala1,3,11,15]-Endothelin (53-63) can be used for the research of vasoconstriction

Methylsolfonyl 25(S)-Δ7-dafachronic acid (compound 3) is a selective ssDAF-12 agonist with the IC₅₀ of 0.41 μM. Methylsolfonyl 25(S)-Δ7-dafachronic acid shows low cell cytotoxicity in HepG2 cells with IC₅₀ of >200 μM. Methylsolfonyl 25(S)-Δ7-dafachronic acid can be used for study of parasitism.

[Lys4] Sarafotoxin S6c, a sarafotoxin analogue, is a potent and partial agonist of endothelin receptor. [Lys4] Sarafotoxin S6c elicits contraction of pig coronary artery, with an EC₅₀ of 1.5 nM.

Sarafotoxin S6a TFA , a sarafotoxin analogue, is a endothelin receptor agonist and has an ET_A/ET_B selectivity profile similar to that of Endothelin-3 (HY-P0204). Sarafotoxin S6a TFA elicits the pig coronary artery with an EC₅₀ value of 7.5 nM.

Sarafotoxin S6b is a vasoconstrictor peptide, and a non-selective endothelin receptor agonist. Sarafotoxin S6b can induce contraction in isolated human coronary arteries , the K_i values of Coronary artery, Saphenous vein and Coronary artery are 0.27, 0.55 and 19.5 nM, respectively.

Endothelin (16-21) is a selective ETB receptor agonist (EC₅₀=228 nM in guinea-pig bronchus). Endothelin (16-21) can induce smooth muscle contraction. Endothelin (16-21) is promising for research of respiratory (e.g., asthma) and cardiovascular (e.g., hypertension) diseases.

[Asn18] Endothelin-1 swine, human is a structural analogue of Endothelin 1 (swine, human) (HY-P0202), with the Asp amino acid at position 18 mutated to Asn. Endothelin 1 (swine, human) is a synthetic peptide with human and porcine endothelin 1 sequences and is a potent endogenous vasoconstrictor.