中文名称: (-)-Blebbistatin
英文名称: (-)-Blebbistatin
CAS No: 856925-71-8
分子式: C18H16N2O2
分子量: 292.33
B10790 (-)-Blebbistatin ≥98% (psaitong)
包装规格:
50mg in glass bottle
溶解性:
溶于DMSO(10mg/mL 超声)
产品描述:

基本信息

产品编号:B10790

产品名称:(-)-Blebbistatin

CAS:

856925-71-8

 

储存条件

 

粉末

2-8℃

四年

分子式:

C18H16N2O2

分子量

292.33

化学名: 

 

 

Solubility (25°C)

 

体外

DMSO

39mg/mL (133.41mM)

Ethanol

Insoluble

Water

Insoluble

体内(现配现用)

2% DMSO+40% PEG 300+5% Tween 80+ddH2O

5mg/mL

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

3.4208mL

17.1040mL

34.2079mL

5mM

0.6842mL

3.4208mL

6.8416mL

10mM

0.3421mL

1.7104mL

3.4208mL

50mM

0.0684mL

0.3421mL

0.6842mL

 

生物活性

产品描述

一种选择性的非肌肉肌球蛋白 II (myosin II) ATPase 活性的抑制剂。

靶点/IC50

non-muscle myosin II ATPases
(Cell-free assay)

0.5 μM-5μM

 

体外研究

Blebbistatin potently inhibits several striated muscle myosins as well as vertebrate nonmuscle myosin IIA and IIB with IC50 values ranging from 0.5 to 5μM. Smooth muscle myosin is only poorly inhibited (IC50=80μM). Blebbistatin does not compete with nucleotide - binding to the skeletal muscle myosin subfragment-1. The inhibitor preferentially binds to the ATPase intermediate with ADP and phosphate bound at the active site, and it slows down phosphate release. It blocks the myosin heads in a products complex with low actin affinity. In culture-activated hepatic stellate cells, blebbistatin is found to change both cell morphology and function. Stellate cells become smaller, acquire a dendritic morphology and have less myosin IIA-containing stress fibres and vinculin-containing focal adhesions. Blebbistatin impairs silicone wrinkle formation,reduces collagen gel contraction and blocks endothelin-1-induced intracellular Ca2+ release. It promotes wound-induced cell migration.

体内研究

Blebbistatin dose-dependently and completely relax both KCl- and carbachol-induced rat detrusor and endothelin-1-induced human bladder contraction. Pre-incubation with 10μM blebbistatin attenuates carbachol responsiveness by 65% while blocking electrical field stimulation-induced bladder contraction reaching 50% inhibition at 32 Hz.

 

推荐实验方法(仅供参考)

激酶实验:

肌动蛋白活化的MgATPase检测

通过NADH耦合检测,使用Beckman DU 640分光光度计测量肌动蛋白活化的MgATPase活性。Blebbistatin[(+)和(-)对映体的外消旋混合物]溶解在DMSO中, 所有样品中DMSO浓度维持在恒定浓度5%。

 

细胞实验:

 

Freshly isolated HSCs are replated on 96-well plate. At day 3, medium is replaced by serum-free medium and cells are starved overnight,treated with or without blebbistatin (25μM) for 2h followed by stimulation with platelet-derived growth factor-BB (20ng/mL).After an overnight incubation, the WST-1 cell proliferation assay are performed.

保存条件:
2-8℃
UN码:
HazardClass:
危害声明:
安全说明:
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参考文献 & 客户发表文献

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

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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

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连续稀释计算器方程

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  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):