Cat. No.: HY-10341B

Fasudil hydrochloride semihydrate

(Synonyms: HA-1077 hydrochloride semihydrate; AT877 hydrochloride semihydrate)

13 Cited Publications

Customer Review

Based on 13 publication(s) in Google Scholar

Fasudil (HA-1077; AT877) hydrochloride semihydrate is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an K_i of 0.33 μM for ROCK1, IC₅₀s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil hydrochloride semihydrate is also a potent Ca²⁺ channel antagonist and vasodilator.

For research use only. We do not sell to patients.

CAS No.: 186694-02-0
Formula: C₁₄H₁₉ClN₃O_2.5S
Molecular Weight:673.68

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (286 KB)

Fasudil hydrochloride semihydrate Chemical Structure

CAS No.: 186694-02-0

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (13)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

PKA

4.58 μM (IC₅₀)

p160ROCK

0.33 μM (Ki)

ROCK2

0.158 μM (IC₅₀)

PKC

12.3 μM (IC₅₀)

PKG

1.65 μM (IC₅₀)

All ROCK Isoforms :

All Calcium Channel Isoforms :

All HIV Isoforms :

All PKA Isoforms :

All PKC Isoforms :

In Vitro

Fasudil hydrochloride semihydrate (100 μM) inhibits cell spreading, the formation of stress fibers, and expression of α-SMA with concomitant suppression of cell growth in rat HSCs (hepatic stellate cells) and human HSC-derived TWNT-4 cells^[4].
Fasudil hydrochloride semihydrate (50-100 μM; 24 hours) inhibits the LPA (lysophoaphatidic acid)-induced phosphorylation of ERK1/2, JNK, and p38 detected by western blotting in rat HSCs and human HSC-derived TWNT-4 cells^[4].
Fasudil hydrochloride semihydrate (25-100 μM; 24 hours) suppresses transcription of collagen and TIMP, stimulates transcription of MMP-1 in human HSC-derived TWNT-4 cells^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[4]

Cell Line:

Rat HSCs and human HSC-derived TWNT-4 cells
Concentration:

50 μM; 100 μM
Incubation Time:

24 hours
Result:

Suppressed the LPA-induced phosphorylation of ERK1/2, JNK and p38 MAPK by 60%, 70%,and 90%, respectively.

RT-PCR^[4]

Cell Line:

Rat HSCs and human HSC-derived TWNT-4 cells
Concentration:

25 μM; 50 μM; 100 μM
Incubation Time:

24 hours
Result:

Reduced the expression of type I collagen, a-SMA, and TIMP-1.

In Vivo

Fasudil hydrochloride semihydrate (10 mg/kg; i.v.; 1 h before operation) exhibits protectable effects on cardiovascular disease and reduces the activation of JNK and attenuates mitochondrial-nuclear translocation of AIF under ischemic injury^[5].
Fasudil hydrochloride semihydrate (50 mg/kg/d; i.p.) inhibits acute and relapsing EAE (experimental autoimmune encephalomyelitis) induced by proteolipid protein PLP p139-151, reduces lymphocytes proliferation, results downregulation of interleukin (IL)-17 and a marked decrease of the IFN-γ/IL-4 ratio^[6].
Fasudil hydrochloride semihydrate (100 mg/kg/d; p.o.) significantly reduces incidence and pathological examination score of EAE (experimental autoimmune encephalomyelitis) in SJL/J mice, decreases inflammation, demyelination, axonal loss and APP positivein spinal cord in mice^[6].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Myocardial ischemia and reperfusion in rat (250-300 g)^[5]
Dosage:

10 mg/kg
Administration:

Intravenous injection; 1 h before operation
Result:

Activated the Rho-kinase, JNK, and resulted AIF translocated to the nucleus.
Inhibited Rho-kinase activity, and reduced myocardial infarct size and heart cell apoptosis.

Chemical Information

CAS No. 186694-02-0
Molecular Weight 673.68
Formula C₁₄H₁₉ClN₃O_2.5S
SMILES

O=S(C1=CC=CC2=C1C=CN=C2)(N3CCNCCC3)=O.[H]Cl.[0.5H2O]
Synonyms

HA-1077 hydrochloride semihydrate; AT877 hydrochloride semihydrate
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (13)

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Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
J Exp Clin Cancer Res

3,3'-Diindolylmethane modulates aryl hydrocarbon receptor of esophageal squamous cell carcinoma to reverse epithelial-mesenchymal transition through repressing RhoA/ROCK1-mediated COX2/PGE2 pathway. [Abstract]

2020 Jun 16;39(1):113. PMID: 32546278
Int J Biol Sci

Angiogenic and Fibrogenic Dual-effect of Gremlin1 on Proliferative Diabetic Retinopathy. [Abstract]

2024 Jan 12;20(3):897-915. PMID: 38250154
Neural Regen Res

Environmental enrichment combined with fasudil promotes motor function recovery and axonal regeneration after stroke. [Abstract]

2021 Dec;16(12):2512-2520. PMID: 33907042
Clin Transl Med

Inhibition of ROCK ameliorates pulmonary fibrosis by suppressing M2 macrophage polarisation through phosphorylation of STAT3. [Abstract]

2022 Oct;12(10):e1036. PMID: 36178087
Clin Transl Med

Functional genomic analysis of epithelioid sarcoma reveals distinct proximal and distal subtype biology. [Abstract]

2022 Jul;12(7):e961. PMID: 35839307
Br J Cancer

Functional genomics of human clear cell sarcoma: genomic, transcriptomic and chemical biology landscape for clear cell sarcoma. [Abstract]

2023 May;128(10):1941-1954. PMID: 36959380
Inflammopharmacology

Diosmetin alleviates acute lung injury caused by lipopolysaccharide by targeting barrier function. [Abstract]

2023 Aug;31(4):2037-2047. PMID: 37074600
Cell Signal

RhoA/ROCK1 aggravates transverse aortic constriction-induced atrial fibrillation by enhancing NF-κBp65/CCL2 signaling pathway. [Abstract]

2026 Feb:138:112275. PMID: 41317932
J Pharm Pharmacol

Fasudil alleviated insulin resistance through promotion of proliferation, attenuation of cell apoptosis and inflammation and regulation of RhoA/Rho kinase/insulin/nuclear factor-κB signalling pathway in HTR-8/SVneo cells. [Abstract]

2021 Jul 7;73(8):1118-1127. PMID: 33779714
Adipocyte

KD025 (SLx-2119) suppresses adipogenesis at intermediate stage in human adipose-derived stem cells. [Abstract]

2019 Dec;8(1):114-124. PMID: 30860936
Preprints

2025 Dec 2.
SSRN

2023 Feb 24.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (286 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Chen M, et al. Fasudil and its analogs: a new powerful weapon in the long war against central nervous system disorders? Expert Opin Investig Drugs. 2013 Apr;22(4):537-50. [Content Brief]

[2]. Huang XN, et al. The effects of fasudil on the permeability of the rat blood-brain barrier and blood-spinal cordbarrier following experimental autoimmune encephalomyelitis. J Neuroimmunol. 2011 Oct 28;239(1-2):61-7. [Content Brief]

[3]. Uehata M, et al. Calcium sensitization of smooth muscle mediated by a Rho-associated protein kinase in hypertension. Nature. 1997 Oct 30;389(6654):990-4. [Content Brief]

[4]. Fukushima M, et al. Fasudil hydrochloride hydrate, a Rho-kinase (ROCK) inhibitor, suppresses collagen production and enhances collagenase activity in hepatic stellate cells. Liver Int. 2005 Aug;25(4):829-38. [Content Brief]

[5]. Zhang J, et al. Inhibition of the activity of Rho-kinase reduces cardiomyocyte apoptosis in heart ischemia/reperfusion via suppressing JNK-mediated AIF translocation. Clin Chim Acta. 2009 Mar;401(1-2):76-80. [Content Brief]

[6]. Sun X, et al. The selective Rho-kinase inhibitor Fasudil is protective and therapeutic in experimental autoimmune encephalomyelitis. J Neuroimmunol. 2006 Nov;180(1-2):126-34. Epub 2006 Sep 22. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Fasudil hydrochloride semihydrate

13 Cited Publications

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Fasudil hydrochloride semihydrate

Publications Citing Use of MedChemExpress (MCE) Fasudil hydrochloride semihydrate

All ROCK Isoforms

All Calcium Channel Isoforms

All HIV Isoforms

All PKA Isoforms

All PKC Isoforms

Biological Activity

Chemical Information

Publications (13)

Purity & Documentation

References

Calculators

Help & FAQs

Fasudil hydrochloride semihydrate Related Classifications

HY-10341B Related Classifications