BQ-3020 (trifluoroacetate salt

肽ETB受体拮抗剂；选择性地与ETB结合，而非ETA受体（IC50s分别为0.07和940nM）；诱导牛颈动脉分离内皮细胞中的肌醇三磷酸形成和钙动员；分别增加或降低Dahl盐抗性大鼠或敏感大鼠的肾灌注压；减少NO生成并诱导饮食诱发的高胆固醇血症大鼠模型中的血管收缩。A peptide ETB receptor antagonist; selectively binds to ETB over ETA receptors (IC50s = 0.07 and 940 nM, respectively); induces inositol triphosphate formation and calcium mobilization in isolated bovine carotid artery endothelial cells; increases or decreases renal perfusion pressure in Dahl salt-resistant or -sensitive rats, respectively; decreases NO production and induces vasoconstriction in a rat model of diet-induced hypercholesterolemia.分子式C96H140N20O25S • XCF3COOH分子量2006.3OC(C=C1)=CC=C1C[C@H](NC([C@H](C(C)C)NC([C@H](C)NC([C@H](CCC(O)=O)NC([C@H](CCCCN)NC([C@H](CC(O)=O)NC([C@H](CCSC)NC([C@@H](NC(C)=O)CC(C)C)=O)=O)=O)=O)=O)=O)=O)C(N[C@@H](CC2=CC=CC=C2)C(N[C@@H](C)C(N[C@@H](CC3=CN=CN3)C(N[C@@H](CC(C)C)C(N[C@@H](CC(O)=O)C(N[C@@H]([C@@H](C)CC)C(N[C@@H]([C@@H](C)CC)C(N[C@H](C(O)=O)CC4=CNC5=CC=CC=C45)=O)=O)=O)=O)=O)=O)=O)=O.OC(C(F)(F)F)=O