|六氢-1-(5-异喹啉磺酰基)-1H-1,4-二氮杂卓盐酸盐|CsnPharm

CAS No.: 105628-07-7

盐酸法舒地尔 Catalog No. CSN10984

Synonyms: HA-1077 Hydrochloride;AT-877 Hydrochloride;HA-1077

Fasudil HCl is a potent inhibitor of ROCK-II, PKA, PKG, PKC, and MLCK with Ki of 0.33 μM, 1.6 μM, 1.6 μM, 3.3 μM and 36 μM, respectively.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 MLCK

Ki:36μM PKA

Ki:1.6μM PKC

Ki:3.3μM PKG

Ki:1.6μM ROCK2

Ki:0.33μM
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

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

更多
动物研究
剂量
Rat: 30 mg/kg^[3] (i.v.), 10 mg/kg^[4] (i.p.) Mice: 100 mg/kg^[3] (p.o.), 50 mg/kg^[5] (i.p.)

给药途径
i.v., p.o., i.p.
临床研究

动物研究
剂量	Rat: 30 mg/kg^[3] (i.v.), 10 mg/kg^[4] (i.p.) Mice: 100 mg/kg^[3] (p.o.), 50 mg/kg^[5] (i.p.)
给药途径	i.v., p.o., i.p.

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 ... more >> Tehran, Iran, Islamic Republic of Collapse <<
NCT00120718	Atherosclerosis ... more >> Hypercholesterolemia Collapse <<	Phase 2	Completed	-	United States, Massachusetts ... more >> Brigham and Women's Hospital Boston, Massachusetts, United States, 02115 Collapse <<
NCT01069042	Heart Failure	Phase 4	Unknown	November 2010	Taiwan ... more >> National Cheng Kung University Hospital Recruiting Tainan, Taiwan, 70401 Contact: Ping-Yen Liu, MD, PhD Collapse <<

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.0504 mL
- 15.2518 mL
- 30.5037 mL
- 5 mM
- 0.6101 mL
- 3.0504 mL
- 6.1007 mL
- 10 mM
- 0.3050 mL
- 1.5252 mL
- 3.0504 mL

技术信息

CAS号

105628-07-7

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C14H18ClN3O2S

运输

蓝冰

分子量

327.83

别名

HA-1077 Hydrochloride;AT-877 Hydrochloride;HA-1077;HA-1077 HCl;Fasudil hydrochloride;盐酸法舒地尔

溶解度

DMSO	200.0 mg/mL (610.1 mM) warming
Water	140.0 mg/mL (427.1 mM)

动物实验配方

0.5% CMC-Na

60 mg/mL

clear

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

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 ... more >> Tehran, Iran, Islamic Republic of Collapse <<
NCT00120718	Atherosclerosis ... more >> Hypercholesterolemia Collapse <<	Phase 2	Completed	-	United States, Massachusetts ... more >> Brigham and Women's Hospital Boston, Massachusetts, United States, 02115 Collapse <<
NCT01069042	Heart Failure	Phase 4	Unknown	November 2010	Taiwan ... more >> National Cheng Kung University Hospital Recruiting Tainan, Taiwan, 70401 Contact: Ping-Yen Liu, MD, PhD Collapse <<
NCT00670202	Carotid Stenosis	Phase 2	Terminated(Slow enrollment)	-	United States, Massachusetts ... more >> Brigham and Women's Hospital Boston, Massachusetts, United States, 02115 Collapse <<
NCT03391219	Retinal Vein Occlusion	Phase 2 Phase 3	Recruiting	October 2018	Iran, Islamic Republic of ... more >> Ophthalmic Research Center Recruiting Tehran, Iran, Islamic Republic of Contact: Ramin Noorinia, MD 009822591616 labbafi@hotmail.com Collapse <<
NCT00498615	Raynaud Scler... more >>oderma Collapse <<	Phase 3	Completed	-	United States, Maryland ... more >> Johns Hopkins University Baltimore, Maryland, United States, 21224 Collapse <<
NCT01935518	Amyotrophic Lateral Sclerosis	Phase 2	Unknown	May 2015	China ... more >> Peking University Third Hospital Recruiting Beijing, China, 100191 Contact: Xiaolu Liu, MD 0086-1082265032 liuxiaolupku@gmail.com Principal Investigator: Dongsheng Fan, MD, PhD Collapse <<
NCT00498615	-	-	Completed	-	-
NCT03753269	ST Segment Elevation Myocardia... more >>l Infarction Collapse <<	Phase 4	Not yet recruiting	December 30, 2022	-
NCT03404843	Cardiovascular Diseases	Phase 2	Completed	-	United States, Colorado ... more >> Colorado State University, Dept. of Health and Exercise Science Fort Collins, Colorado, United States, 80523 Collapse <<
NCT00670202	-	-	Terminated(Slow enrollment)	-	-

靶点	Description	IC50
MLCK		Ki:36μM
PKA		Ki:1.6μM
PKC		Ki:3.3μM
PKG		Ki:1.6μM
ROCK2		Ki:0.33μM

盐酸法舒地尔 Catalog No. CSN10984

靶点选择性

请登录您的专属账户

确认信息