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BQ-788 sodium salt
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BQ-788 sodium salt
CAS No. : 156161-89-6
MCE 站:BQ-788 sodium salt
产品活性:BQ-788 sodium salt 是一种有效,选择性的 ETB 受体拮抗剂,在人类 Girrardi 心脏细胞中抑制 ET-1 与 ETB 受体结合的 IC50 为 1.2 nM。
研究领域:GPCR/G Protein
作用靶点:Endothelin Receptor
In Vitro: BQ-788 potently and competitively inhibits 125I-labeled ET-1 binding to ETB receptors in human Girrardi heart cells with an IC50 of 1.2 nM, but only poorly inhibits the binding to ETA receptors in human neuro-blastoma cell line SK-N-MC cells (IC50, 1300 nM). BQ-788 shows no agonistic activity up to 10 μM and competitively inhibits thevasoconstriction induced by an ETB-selective agonist (pA2, 8.4). BQ-788 also inhibits several bioactivities of ET-1, such as bronchoconstriction, cell proliferation, and clearance of perfused ET-1.
In Vivo: BQ-788 (3 mg/kg/h, i.v.) completely inhibits a pharmacological dose of ET-1- or sarafotoxin6c (0.5 nmol/kg, i.v.)-induced ETB receptor-mediated depressor, but not pressor responses in conscious rats. Furthermore, BQ-788 markedly increases the plasma concentration of ET-1, which is considered an index of potential ETB receptor blockade in vivo. In Dahl salt-sensitive hypertensive (DS) rats, BQ-788 (3 mg/kg/h, i.v.) increases blood pressure by about 20 mm Hg. It is reported that BQ-788 also inhibits ET-1-induced bronchoconstriction, tumor growth and lipopolysaccharide-induced organfailure. BQ 788 (3 mg/kg) results in an eightfold leftward shift in the ET-1 dose-response curve, suggesting a significant involvement of ETB dilator receptors. Mice are treated with 30 nmol BQ-788 by intraplantar, reduce mechanical hyperalgesia (47% and 42%), thermal hyperalgesia (68% and 76%), oedema (50% and 30%); myeloperoxidase activity (64% and 32%), and overt-pain like behaviours. Additionally, intraplantar treatment with clazosentan or BQ-788 decreases spinal (45% and 41%) and peripheral (47% and 47%) superoxide anion production as well as spinal (47% and 47%) and peripheral (33% and 54%) lipid peroxidation, respectively.
相关产品:Clinical Compound Library Plus | Bioactive Compound Library Plus | Peptidomimetic Library | Endothelin 1 (swine, human) | Bosentan | BQ-123 | Atrasentan hydrochloride | Sparsentan | Ambrisentan | Atrial Natriuretic Peptide (ANP) (1-28), human, porcine Acetate | Sulfisoxazole | Atrial Natriuretic Peptide (ANP) (1-28), rat | Avosentan | Zibotentan | Darusentan | Sitaxsentan sodium | A-192621 | IRL 2500 | BQ-3020 TFA | IRL-1620 | Nebentan | Tezosentan | ABT-546 | Aminaftone | Aprocitentan D4 | BMS-248360 | BQ-788
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