化合物BQ-788 T10595
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
TargetMol | 生产商 | 美国 | 现货 |
性能特点
生化试剂,可用于动物细胞实验
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
10 mg | 173326-37-9 | ¥3,850.00 | 询底价 |
1 mL | 173326-37-9 | ¥2,970.00 | 询底价 |
1 mg | 173326-37-9 | ¥1,230.00 | 询底价 |
2 mg | 173326-37-9 | ¥1,730.00 | 询底价 |
5 mg | 173326-37-9 | ¥2,680.00 | 询底价 |
50 mg | 173326-37-9 | ¥8,230.00 | 询底价 |
25 mg | 173326-37-9 | ¥5,970.00 | 询底价 |
100 mg | 173326-37-9 | ¥10,900.00 | 询底价 |
Product Introduction
Bioactivity
英文名: BQ-788
描述: BQ-788 是一种具有选择性和有效性的 ETB 受体拮抗剂,具有潜在的高血压活性,抑制 ET-1 与 ETB 受体结合,抑制外源性 ET-1 诱导的冠状动脉灌注压升高。
体外活性: BQ-788 potently and competitively inhibits the binding of 125I-labeled ET-1 to ETB receptors in human Girrardi heart cells (hGH) with an IC50 of 1.2 nM. However, it poorly inhibits the binding to ETA receptors in the human neuroblastoma cell line SK-N-MC cells (IC50, 1300 nM). BQ-788, up to 10 μM, shows no agonistic activity and competitively inhibits the vasoconstriction induced by an ETB-selective agonist (pA2, 8.4). Additionally, BQ-788 inhibits several bioactivities of ET-1, such as bronchoconstriction, cell proliferation, and clearance of perfused ET-1[1].
体内活性: In conscious rats, BQ-788 (3 mg/kg/h, i.v.) completely inhibits ETB receptor-mediated depressor responses induced by a pharmacological dose of ET-1 or sarafotoxin6c (0.5 nmol/kg, i.v.), but not pressor responses. Additionally, BQ-788 markedly increases the plasma concentration of ET-1, 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.) raises blood pressure by about 20 mm Hg. It is reported that BQ-788 also inhibits ET-1-induced bronchoconstriction, tumor growth, and lipopolysaccharide-induced organ failure[1]. BQ 788 (3 mg/kg) results in an eightfold leftward shift in the ET-1 dose-response curve, suggesting significant involvement of ETB dilator receptors[2]. In mice treated with 30 nmol BQ-788 by intraplantar administration, there is a reduction in mechanical hyperalgesia (47% and 42%), thermal hyperalgesia (68% and 76%), oedema (50% and 30%), myeloperoxidase activity (64% and 32%), and overt-pain like behaviors. 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[3].
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 150 mg/mL (233.72 mM)
关键字: BQ 788 | BQ-788
相关产品: Bosentan (hydrate) | Endothelin 1 (swine, human) acetate | IRL-1620 acetate | Atrasentan hydrochloride | Sulfisoxazole | Ambrisentan | Ro 46-2005 | Avosentan | Sitaxsentan | Carperitide acetate
相关库: Drug Repurposing Compound Library | Membrane Protein-targeted Compound Library | GPCR Compound Library
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注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途