中文名称: | BQ-788 | ||||
---|---|---|---|---|---|
英文名称: | BQ-788 | ||||
CAS No: | 173326-37-9 | 分子式: | C34H51N5O7 | 分子量: | 641.8 |
CAS No: | 173326-37-9 | ||||
分子式: | C34H51N5O7 | ||||
分子量: | 641.8 |
基本信息
产品编号: |
B10870 |
||||
产品名称: |
BQ-788 |
||||
CAS: |
173326-37-9 |
储存条件 |
粉末 |
-20℃ |
四年 |
分子式: |
溶于液体 |
-80℃ |
二年 |
||
分子量: |
641.80 |
|
|
||
化学名: |
|||||
Solubility (25°C): |
|||||
体外:
|
DMSO |
|
|||
Ethanol |
|
||||
Water |
|
||||
体内(现配现用): |
|
||||
<1mg/ml表示微溶或不溶。 |
|||||
普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 |
|||||
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
1.5581mL |
7.7906mL |
15.5812mL |
5mM |
0.3116mL |
1.5581mL |
3.1162mL |
10mM |
0.1558mL |
0.7791mL |
1.5581mL |
生物活性
产品描述 |
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1.2nM。 |
靶点 |
IC50:1.2nM (ETB) |
体外研究 |
BQ-788 potently and competitively inhibits 125I-labeled ET-1 binding to ETB receptors in human Girrardi heart cells (hGH) with an IC50 of 1.2nM,but only poorly inhibits the binding to ETA receptors in human neuro-blastoma cell line SK-N-MC cells (IC50,1300nM).BQ-788 shows no agonistic activity up to 10μM 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. |
体内研究 |
BQ-788 (3mg/kg/h,i.v.) completely inhibits a pharmacological dose of ET-1- or sarafotoxin6c (0.5nmol/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 (3mg/kg/h,i.v.) increases blood pressure by about 20mm Hg.It is reported that BQ-788 also inhibits ET-1-induced bronchoconstriction,tumor growth and lipopolysaccharide-induced organfailure.BQ 788 (3mg/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 30nmol 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. |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )