156161-89-6
基本信息
BQ-788 SODIUM
BQ789 Sodium Salt
1-ELAIDYLPHOSPHOCHOLINE, >97%
BQ788 SODIUM SALT
BQ 788 SODIUM SALT
BQ-788 SYNTHETIC >97% ETB ENDOTHELIN REC EPT
N-[N-[N-[(2,6-Dimethyl-1-piperidinyl)carbonyl]-
N-cis-2,6-dimethylpiperidinocarbonyl-L-γMeLeu-D-Trp(COOMe)-D-Nle-ONa
2,6-Dimethylpiperidinecarbonyl-γ-Methyl-Leu-Nin-(Methoxycarbonyl)-D-Trp-D-Nle
DMpc-gaMMa-MeLeu-D-Trp(1-CO2CH3)-D-Nle.Na (DMpc : cis-2,6-DiMethylpiperidinocarbonyl)
物理化学性质
| 储存条件 | -20°C |
| 溶解度 | acetonitrile: 0.3 mg/mL |
| 溶解度 | 在乙腈中的溶解度：0.3 mg/mL |
| 形态 | solid |
| 颜色 | white |
| 水溶解性 | acetonitrile: 0.3mg/mL DMSO: 1.2mg/mL ethanol: 1.2mg/mL H2O: slightly soluble |
安全数据
| 危险性符号(GHS) |  GHS07 |
| 警示词 | 警告 |
| 危险性描述 | H302-H315-H319-H335 |
| 防范说明 | P261-P280-P301+P312-P302+P352-P305+P351+P338 |
| WGK Germany | 3 |
| WGK Germany | 3 |
常见问题列表
IC50: 1.2 nM (ETB)
BQ-788 potently and competitively inhibits 125 I-labeled ET-1 binding to ETB receptors in human Girrardi heart cells with an IC 50 of 1.2 nM, but only poorly inhibits the binding to ETA receptors in human neuro-blastoma cell line SK-N-MC cells (IC 50 , 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.
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.