Fasudil HCl
产品说明书
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同义名 : | HA-1077 Hydrochloride;AT-877 Hydrochloride;Fasudil HCl |
| CAS号 : | 105628-07-7 | |
| 货号 : | A193859 | |
| 分子式 : | C14H18ClN3O2S | |
| 纯度 : | 98% | |
| 分子量 : | 327.83 | |
| MDL号 : | - | |
| 存储条件： |
Pure form Keep in dark place,Inert atmosphere,Room temperature In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 30 mg/mL(91.51 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO H2O: 55 mg/mL(167.77 mM)，配合低频超声助溶 |
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| 动物实验配方： |
PO 0.5% CMC-Na 60 mg/mL clear |
| 生物活性 | |||
|---|---|---|---|
| 靶点 |
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| 描述 | Fasudil Hydrochloride is the hydrochloride form of Fasudil with higher solubility. Fasudil is a selective Rock inhibitor with Ki value of 0.33μM, as well as showed inhibitory activity against Protein kinase A, Protein kinase G, Protein kinase C, MLCK with Ki values of 1.6μM, 1.6μM, 3.3μM and 36μM. Addition of 0.3-100μM Fasudil could dose-dependently inhibited Ca2+ sensitization of force in guinea-pig ileum. Treatment with fasudil significantly suppressed LCc-EC migration, which may due to its impaction on polymerization of the cytoskeletal actin filament network. Incubation with Fasudil at concentration ranging in 1-100μM in MDA-MB-231 cell colonies for 21 days could concentration-dependently inhibit the the anchorage-independent cell growth in a soft agar assay. In an orthotopic MDA-MB-231 rat model, fasudil did not suppress growth of established tumors, but could greatly reduce the incidence of tumor formation through oral administration at dose of 200 mg/kg/day or continuously in the drink at dose of ~228 mg/kg/day. | ||
| 细胞研究 | |||||
|---|---|---|---|---|---|
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活性说明 | 数据源 |
| HEK293 cells | Function assay | Inhibition of His-tagged human PRK2 expressed in HEK293 cells, IC50=4 μM. | 10998351 | ||
| insect cells | Function assay | 10 mins | Inhibition of human leukocytic ROCK1 expressed in insect cells using KKRNRTLSV as substrate after 10 mins by pyruvate kinase/lactate dehydrogenase coupled assay, Ki=0.53 μM. | 26039570 | |
| Sf9 cells | Function assay | 90 mins | Inhibition of human recombinant N-terminal his-tagged ROCK1 (3-543) expressed in baculovirus infected Sf9 cells using Biotin-Ahx-AKRRLSSLRA-CONH2 substrate and [gamma-33P]ATP after 90 mins by scintillation proximity assay, IC50=0.3 μM. | 17018693 | |
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT01823081 | Diabetic Macular Edema | Phase 3 | Completed | - | Iran, Islamic Republic of ... 展开 >> Tehran, Iran, Islamic Republic of 收起 << |
| NCT00120718 | Atherosclerosis ... 展开 >> Hypercholesterolemia 收起 << | Phase 2 | Completed | - | United States, Massachusetts ... 展开 >> Brigham and Women's Hospital Boston, Massachusetts, United States, 02115 收起 << |
| NCT01069042 | Heart Failure | Phase 4 | Unknown | November 2010 | Taiwan ... 展开 >> National Cheng Kung University Hospital Recruiting Tainan, Taiwan, 70401 Contact: Ping-Yen Liu, MD, PhD 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
3.05mL 0.61mL 0.31mL |
15.25mL 3.05mL 1.53mL |
30.50mL 6.10mL 3.05mL |
