DC Chemicals supplies: BQ-788,cas: 156161-89-6,Catalog: DC7542,In stock.
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Product name: BQ-788, Synonyms: BQ788 sodium salt; BQ 788 sodium salt, cas: 156161-89-6, MW: 663.78, Molecule Formula: C34H50N5NaO7
BQ-788, cas 156161-89-6, Purity>98%. Best price and quality from DC Chemicals. Balapiravir (R1626, Ro 4588161) is the prodrug of a nucleoside analogue inhibitor of the hepatitis C virus (HCV) RNA-dependent RNA polymerase (R1479, RG1479).
BQ-788 sodium salt is a potent, selective ETB receptor antagonist (IC50 = 1.2 nM For inhibition of ET-1 binding to human Girardi heart cells); poorly inhibited the binding to ET A receptors in human neuroblastoma cell line SK-N-MC cells (IC(50), 1300 nM).
IC50 value: 1.2 nM
Target: ETB receptor
in vitro: BQ-788 potently and competitively inhibited (125)I-labeled ET-1 binding to ET(B) receptors in human Girrardi heart cells (hGH) with an IC(50) of 1.2 nM, but only poorly inhibited the binding to ET A receptors in human neuroblastoma cell line SK-N-MC cells (IC(50), 1300 nM). In isolated rabbit pulmonary arteries, BQ-788 showed no agonistic activity up to 10 microM and competitively inhibited the vasoconstriction induced by an ET(B)-selective agonist (pA(2), 8.4). BQ-788 also inhibited several bioactivities of ET-1, such as bronchoconstriction, cell proliferation, and clearance of perfused ET-1. In the rat aorta, BQ-788 antagonized the endothelium-dependent, ETB1 receptor-mediated relaxation due to endothelin (ET)-3 with EC50 of 3 microM. In the rat aorta without endothelium, 10 microM BQ-788 weakly antagonized the ETA1-mediated contractile effects of ET-1 and ET-3 .
in vivo: In conscious rats, BQ-788, 3 mg/kg/h, i.v., completely inhibited a pharmacological dose of ET-1- or sarafotoxin6c (S6c) (0.5 nmol/kg, i.v.)-induced ET(B) receptor-mediated depressor, but not pressor responses. Furthermore, BQ-788 markedly increased the plasma concentration of ET-1, which is considered an index of potential ET(B) receptor blockade in vivo. In Dahl salt-sensitive hypertensive (DS) rats, BQ-788, 3 mg/kg/h, i.v., increased blood pressure by about 20 mm Hg. It is reported that BQ-788 also inhibited ET-1-induced bronchoconstriction, tumor growth and lipopolysaccharide-induced organ failure. BQ 788 (3 mg/kg) resulted in an eightfold leftward shift in the ET-1 dose-response curve, suggesting a significant involvement of ETB dilator receptors. In the absence or presence of BQ 788, each ET antagonist evoked a rightward shift from vehicle. With the exception of BMS 182874, BQ 788 increased the magnitude of the shifts.For the detailed information of BQ-788, the solubility of BQ-788 in water, the solubility of BQ-788 in DMSO, the solubility of BQ-788 in PBS buffer, the animal experiment (test) of BQ-788, the cell expriment (test) of BQ-788, the in vivo, in vitro and clinical trial test of BQ-788, the EC50, IC50,and Affinity of BQ-788, Please contact DC Chemicals.
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