BQ-123

BQ-123 is a peptide endothelin type A (ETA) receptor antagonist (IC50 = 7.3 nM). It is selective for ETA over ETB receptors (Kis = 0.025 and 31 µM, respectively). BQ-123 inhibits growth of human pulmonary artery smooth muscle cells induced by endothelin-1 (ET-1, Cay-24127). It reverses ET-1-induced increases in mean arterial pressure (MAP) in rats. BQ-123 (3 mg/kg, i.v.) also delays seizure onset and reduces the number of rats with major seizures in a model of epilepsy induced by pentylenetetrazole (PTZ, Cay-18682).Formal Name: cyclo(D-alpha-aspartyl-L-prolyl-D-valyl-L-leucyl-D-tryptophyl). CAS Number: 136553-81-6. Synonyms: Cyclo(D-Trp-D-Asp-Pro-D-Val-Leu). Molecular Formula: C31H42N6O7. Formula Weight: 610.7. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 1 mg/ml, DMSO: 20 mg/ml, DMSO:PBS (pH 7.2) (1:2): 0.33 mg/ml, PBS (pH 7.2): slightly. lambdamax: 221 nm. SMILES: O=C([C@@H](CC1=CNC2=CC=CC=C12)NC([C@H](CC(C)C)NC([C@@H](C(C)C)N3)=O)=O)N[C@]([H])(CC(O)=O)C(N4CCC[C@]4(C3=O)[H])=O. InChi Code: InChI=1S/C31H42N6O7/c1-16(2)12-21-27(40)33-22(13-18-15-32-20-9-6-5-8-19(18)20)28(41)35-23(14-25(38)39)31(44)37-11-7-10-24(37)29(42)36-26(17(3)4)30(43)34-21/h5-6,8-9,15-17,21-24,26,32H,7,10-14H2,1-4H3,(H,33,40)(H,34,43)(H,35,41)(H,36,42)(H,38,39)/t21-. InChi Key: VYCMAAOURFJIHD-PJNXIOHISA-N.