- ￥997 - 4650
- MedChemExpress(MCE)
- 美国
- HY-15894A
- 2025年12月05日
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- 文献和实验
- 技术资料
- 保存条件：
-20°C, sealed storage, away from moisture
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
173326-37-9
- 规格：
10 mM * 1 mL/1 mg/5 mg/10 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥4596.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥997.0 |
| 规格： | 5 mg | 产品价格： | ￥3255.0 |
| 规格： | 10 mg | 产品价格： | ￥4650.0 |
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BQ-788
CAS No. : 173326-37-9
MCE 国际站：BQ-788
产品活性：BQ-788 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 (hGH) 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.
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文献和实验.350.06050.0 2、放射性测定单位单位定义换算吸收放射线剂量（拉得rad）100尔格/克（电离辐射传给单位质量物质的能量）0.87rad=1r伦琴（r）使1克空气产生1.6×1012离子对的X或γ-射线的照射剂量r/0.87=1rad居里（Ci）每秒放射性衰变3.7×1010个原子的量1Ci=103mCi=106μCi毫居（mCi）千分之一居里1mCi=10-3Ci=103μCi微居（μCi）百万分之一居里（每分钟衰变2.2×106次）1μCi=10-6Ci=10-3MCi伯克莱尔（Bq
） =2.22×106 d . p . m .1 nanoCurie （nCi） = 2.22×103 d . p . m .1 picoCurie （pCi） =2.22 d . p . m .1 Ci = 3.7×1010 Bq =37GBq （gigaBq）1 mCi = 3.7×10 7 Bq =37MBq （megaBq）1 m Ci = 3.7×10 4 Bq =37kBq （kiloBq）1 GBq =2.7×10 -4 Ci =27.027mCi（milliCi）1 MBq =2.7×10
度），阴性对照孔不加IL-2。 4．每孔加0.1ml细胞悬液，在37℃ 5％ CO2的饱和水汽二氧化碳培养箱中培养18～24小时。每孔加10μl（0.5μCi或1.85×104Bq）[3H]脱氧胸苷，继续培养4小时。 5．用多头细胞收集器将细胞收集到玻璃纤维滤纸上，用3％醋酸水溶液滤纸3次，洗去游离的[3H]TdR。将滤纸置液体闪烁瓶中，加入5ml闪烁液。在液体闪烁仪上计数细胞摄入的同位素活性（每分钟放射性计数，cpm），根据仪器效率换算成dpm（每分钟衰变数）。
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