Fasudil (HA-1077) HCl

Catalog No.S1573 Synonyms: AT-877

For research use only.

Fasudil (HA-1077, AT-877), a potent and selective inhibitor of Rho kinase, displays less potent inhibiton over PKA, PKG, PKC and MLCK with Ki of 1.6, 1.6, 3.3, and 36 μM in cell-free assays, respectively. Fasudil is also a calcium channel blocker.

Fasudil (HA-1077) HCl Chemical Structure

CAS No. 105628-07-7

Selleck's Fasudil (HA-1077) HCl has been cited by 73 publications

Purity & Quality Control

Choose Selective ROCK Inhibitors

Other ROCK Products

Biological Activity

Description Fasudil (HA-1077, AT-877), a potent and selective inhibitor of Rho kinase, displays less potent inhibiton over PKA, PKG, PKC and MLCK with Ki of 1.6, 1.6, 3.3, and 36 μM in cell-free assays, respectively. Fasudil is also a calcium channel blocker.
Targets
Rho [1] Calcium channel [2] ROCK2 [1]
(Cell-free assay)
PKA [1]
(Cell-free assay)
PKG [1]
(Cell-free assay)
Click to View More Targets
330 nM(Ki) 1.6 μM(Ki) 1.6 μM(Ki)
In vitro

Fasudil is a class of calcium antagonists. Fasudil produces a competitive inhibition of the Ca2+-induced contraction of the depolarized rabbit aorta. Fasudil is able to inhibit contractile responses to KCl, phenylephnne (PHE) and prostaglandin (PG) F2a. [2] Fasudil also exhibits vasodilator actions by inhibition of 5-hydroxytryptamine, noradrenaline, histamine, angiotensin, and dopamine induced spiral strips contraction. [3] Fasudil induces disorganization of actin stress fiber and cell migration inhibition. [4] Fasudil inhibits hepatic stellate cells spreading, the formation of stress fibers, and expression of α-SMA with concomitant suppression of cell growth, but does not induce apoptosis. Fasudil suppresses the LPA-induced phosphorylation of ERK1/2, JNK and p38 MAPK. [5]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
U937 cells MYXGeY5kfGmxbjDhd5NigQ>? MofFTY5pcWKrdHnvckBw\iCPQ2CxMYlv\HWlZXSgZ4hmdW:2YYjpd{BqdiCXOUO3JINmdGy|IH;2[ZJmgHC{ZYPzbY5oKEOFUkKsJGlEPTB;M{Wg{txONg>? NFvLeYg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{C4OFA5Pyd-MUewPFQxQDd:L3G+
Sf9 cells NVHWOZdqTnWwY4Tpc44h[XO|YYm= NXX4bJA2UW6qaXLpeIlwdiCxZjDIbZMufGGpZ3XkJIh2dWGwIF3TT|Eh\XiycnXzd4VlKGmwIGPmPUBk\WyuczygTWM2OD13IN88UU4> MnT0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTB7OUizOVEoRjFyOUm4N|UyRC:jPh?=
HEK293 cells MlTDSpVv[3Srb36gZZN{[Xl? MYPJcohq[mm2aX;uJI9nKEircz30ZYdo\WRiaIXtZY4hWFKNMjDlfJBz\XO|ZXSgbY4hUEWNMkmzJINmdGy|LDDJR|UxRTRizszNMi=> M4nHeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzFyOUm4N|UyLz5zMEm5PFM2OTxxYU6=
Sf9 cells NUi3SW1bTnWwY4Tpc44h[XO|YYm= NFzwUZRKdmirYnn0bY9vKG:oIILheEBTV0ONMjDlfJBz\XO|ZXSgbY4hW2Z7IHPlcIx{NCCLQ{WwQVEvQSEQvF2u MnHtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTB7OUizOVEoRjFyOUm4N|UyRC:jPh?=
insect cells M1PlVmZ2dmO2aX;uJIF{e2G7 M13vXlExKG2rboO= M2fRXGlvcGmkaYTpc44hd2ZiaIXtZY4hdGW3a3;jfZRq[yCUT1PLNUBmgHC{ZYPz[YQhcW5iaX7z[YN1KGOnbHzzJJV{cW6pIFvLVm5TXEyVVjDhd{B{fWK|dILheIUh[W[2ZYKgNVAhdWmwczDifUBxgXK3dnH0[UBscW6jc3WvcIFkfGG2ZTDk[Yh6\HKxZ3XuZZNmKGOxdYDs[YQh[XO|YYmsJGtqRTBwNUOg{txONg>? NGXHcnQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkCzPVU4OCd-Mk[wN|k2PzB:L3G+
Sf9 cells NXHufIJmTnWwY4Tpc44h[XO|YYm= M3fpdVkxKG2rboO= NU\XVmFIUW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDOMZRmem2rbnHsJIhqey22YXfn[YQhWk:FS{GgLFMuPTR|KTDlfJBz\XO|ZXSgbY4h[mGldXzveolzfXNiaX7m[YN1\WRiU3[5JINmdGy|IIXzbY5oKEKrb4Tpck1CcHhvQVvSVmxUW0yUQT3DU25JOiC|dXLzeJJifGViYX7kJHto[W2vYT2zN3BeSVSSIHHmeIVzKDlyIH3pcpMh[nlic3PpcpRqdGyjdHnvckBxem:6aX3peJkh[XO|YYmsJGlEPTB;MD6zJO69VS5? NFHiS2E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zN{CxPFY6Oyd-MUewNVg3QTN:L3G+
A673 NELjVYxyUFSVIHHzd4F6 MlHjdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEF4N{OgZ4VtdHN? MoXyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Assay
Methods Test Index PMID
Western blot ROCK2 / p-ROCK2 / MLC2 / p-MLC2 ; ABCG2 ; Moesin / p-Moesin / β-catenin / p-β-catenin 29416017
Immunofluorescence p-ROCK2 / ABCG2 29416017
Growth inhibition assay Cell viability 29262624
In vivo Intra-coronary injection of Fasudil to dogs (30 μg i.a.) produces an approximate 50% increase in CBF. Fasudil (0.01, 0.03, 0.1 and 0.3 mg/kg, bolus, i.v.) dose-dependently decreases MBP and increases HR, VBF, CBF, RBF, and FBF. A total dose of 1.0 ng/mL Fasudil increases cardiac output. The infusion of Fasudil i.v. produces a significant fall in MBP, left ventricular systolic pressure and total peripheral resistance with an increase in HR and cardiac output, but without significant changes in right atrial pressure, dP/dt or left ventricular minute work in dogs. [3] Fasudil administration displays protectable effects on cardiovascular disease and reduces the activation of JNK and attenuates mitochondrial-nuclear translocation of AIF under ischemic injury. [6] The oral administration of Fasudil (a dosage of 100 mg/kg/day) significantly reduces incidence and mean maximum clinical score of EAE in SJL/J mice immunized with PLP p139-151. Treatment of mice with Fasudil suppresses the proliferative response of splenocytes to the antigen. Oral administration of Fasudil decreases inflammation, demyelination, axonal loss and APP positivein spinal cord of Fasudil-treated mice. [7]

Protocol (from reference)

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
Saline
For best results, use promptly after mixing.

30 mg/mL

Chemical Information

Molecular Weight 327.83
Formula

C14H17N3O2S.HCl

CAS No. 105628-07-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CNCCN(C1)S(=O)(=O)C2=CC=CC3=C2C=CN=C3.Cl

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Fasudil (HA-1077) HCl | Fasudil (HA-1077) HCl supplier | purchase Fasudil (HA-1077) HCl | Fasudil (HA-1077) HCl cost | Fasudil (HA-1077) HCl manufacturer | order Fasudil (HA-1077) HCl | Fasudil (HA-1077) HCl distributor