CAS NO: | 856925-71-8 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
生物活性 | (-)-Blebbistatin is a selective inhibitor of the ATPase activity of non-musclemyosinII[1][2]. | ||||||||||||||||
IC50& Target | IC50: 0.5 to 5 μM (myosin II)[1] | ||||||||||||||||
体外研究 (In Vitro) | Blebbistatin potently inhibits several striated muscle myosins as well as vertebrate nonmuscle myosin IIA and IIB with IC50values ranging from 0.5 to 5 μM. Smooth muscle myosin is only poorly inhibited (IC50=80 μM)[1]. 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[2]. 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[3]. | ||||||||||||||||
体内研究 (In Vivo) | Blebbistatin dose-dependently and completely relax both KCl- and carbachol-induced rat detrusor and endothelin-1-induced human bladder contraction. Pre-incubation with 10 μM blebbistatin attenuates carbachol responsiveness by 65% while blocking electrical field stimulation-induced bladder contraction reaching 50% inhibition at 32 Hz[4]. | ||||||||||||||||
分子量 | 292.33 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C18H16N2O2 | ||||||||||||||||
CAS 号 | 856925-71-8 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 | 4°C, stored under nitrogen *该产品在溶液状态不稳定,建议您现用现配,即刻使用。 | ||||||||||||||||
溶解性数据 | In Vitro: DMSO : 10 mg/mL(34.21 mM;Need ultrasonic) H2O :< 0.1 mg/mL(insoluble) 配制储备液
* 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;该产品在溶液状态不稳定,建议您现用现配,即刻使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百
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