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Chemical Structure| 105628-07-7 Chemical Structure| 105628-07-7

Structure of Fasudil HCl
CAS No.: 105628-07-7

Chemical Structure| 105628-07-7

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Fasudil (HA-1077; AT877) Hydrochloride is a nonspecific RhoA/ROCK inhibitor that also inhibits protein kinases with a Ki of 0.33 μM for ROCK1 and IC50s of 0.158 μM for ROCK2, 4.58 μM for PKA, 12.30 μM for PKC, and 1.650 μM for PKG. Fasudil Hydrochloride is also a potent Ca2+ channel antagonist and vasodilator.

Synonyms: HA-1077 Hydrochloride; AT-877 Hydrochloride; Fasudil(Hydrochloride)

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Product Details of Fasudil HCl

CAS No. :105628-07-7
Formula : C14H18ClN3O2S
M.W : 327.83
SMILES Code : O=S(N1CCNCCC1)(C2=CC=CC3=C2C=CN=C3)=O.[H]Cl
Synonyms :
HA-1077 Hydrochloride; AT-877 Hydrochloride; Fasudil(Hydrochloride)
MDL No. :MFCD00943198
InChI Key :LFVPBERIVUNMGV-UHFFFAOYSA-N
Pubchem ID :163751

Safety of Fasudil HCl

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of Fasudil HCl

epigenetics
cytoskeleton

Isoform Comparison

Biological Activity

Target
  • ROCK2

    ROCK2, Ki:330 nM

  • Calcium Channel

In Vitro:

Cell Line
Concentration Treated Time Description References
mouse embryonic fibroblasts (MEFs) 10μM 30 min Fasudil reduced the relative traction stress of Acvr1R206H/+ cells on 10kPa to levels by Acvr1+/+ cells. PMC7209824
primary cultured microglia isolated from the spinal cord 41 μM 6 h To investigate the effect of Fasudil on microglial migration, the results showed that Fasudil significantly increased the number of migrating microglia. PMC5950678
MCF10A cells 10 μM 24 h To assess the effect of Fasudil on cell viability, results showed that Fasudil treatment did not affect cell viability. PMC7316573
HEL cells 30 μM 5 days To evaluate the effects of Fasudil on IFNα-induced anti-proliferative responses, the results showed that Fasudil in combination with IFNα significantly reduced the viability of HEL cells. PMC8975834
primary PBMCs from PV patients 30 μM To evaluate the effects of Fasudil on IFNα-induced anti-clonogenic responses, the results showed that Fasudil enhanced the suppressive effects of IFNα on primitive malignant erythroid precursors from PV patients who responded poorly to IFN treatment. PMC8975834
cardiomyocytes 100 μM To investigate the effect of Fasudil on mitochondrial function in cardiomyocytes by inhibiting Rock1 expression PMC11700182
Human embryonic stem cells 10 µM Used for removal of the inserted provirus PMC7013232

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
mice Ras-expressing Ptf1a-CreERTM; KRasLSL-G12D adult mice intra-peritoneal injections 10 mg/kg four times each week, until sacrifice Fasudil administration abolished any emergence of neoplasia and blunted YAP/TAZ nuclear accumulation, correlating with normalization of cellular tension as visualized by pMLC. PMC7316573
Mice KPC pancreatic cancer model Oral 2 mg/mouse Daily for 2 weeks Fasudil treatment significantly reduced the invasion of KPC tumor cells into healthy pancreatic tissue, but did not affect tumor cell proliferation. PMC6005347
mice Jak2V617F KI bone marrow transplantation model intraperitoneal injection 25 mg/kg four times per week for 4 weeks To evaluate the effects of Fasudil in combination with PEG-IFNα treatment in a MPN mouse model, the results showed that Fasudil blocked PEG-IFNα-induced ROCK1/2 activation and enhanced the anti-neoplastic effects of PEG-IFNα. PMC8975834
mice Doxorubicin-induced cardiomyopathy model intraperitoneal injection 10 mg/kg once daily for 6 days To investigate the protective effect of Fasudil against Doxorubicin-induced cardiomyopathy by inhibiting Rock1 expression PMC11700182
mice MPD model intraperitoneal 25 mg/kg every 24 hours for 21 days ROCK inhibitors significantly prolonged the survival of mice bearing KITD814V or FLT3N51 and reduced spleen and liver weights. PMC3207244
Mice Ang II infusion model Drinking water 30 mg/kg Once daily for 14 days Fasudil treatment significantly inhibited Ang II-induced VSMC migration and dedifferentiation, and increased the expression of VSMC differentiation markers. PMC7432407

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01823081 Diabetic Macular Edema Phase 3 Completed - Iran, Islamic Republic of ... More >> Tehran, Iran, Islamic Republic of Less <<
NCT00120718 Atherosclerosis ... More >> Hypercholesterolemia Less << Phase 2 Completed - United States, Massachusetts ... More >> Brigham and Women's Hospital Boston, Massachusetts, United States, 02115 Less <<
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 Less <<
NCT00670202 Carotid Stenosis Phase 2 Terminated(Slow enrollment) - United States, Massachusetts ... More >> Brigham and Women's Hospital Boston, Massachusetts, United States, 02115 Less <<
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 Less <<
NCT00498615 Raynaud Scler... More >>oderma Less << Phase 3 Completed - United States, Maryland ... More >> Johns Hopkins University Baltimore, Maryland, United States, 21224 Less <<
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 Less <<
NCT00498615 - Completed - -
NCT03753269 ST Segment Elevation Myocardia... More >>l Infarction Less << 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 Less <<
NCT00670202 - Terminated(Slow enrollment) - -

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.05mL

0.61mL

0.31mL

15.25mL

3.05mL

1.53mL

30.50mL

6.10mL

3.05mL

 

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