Art. -Nr.: HY-10341

Fasudil Hydrochloride

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

29 Cited Publications

Kundenbewertung

Based on 29 publication(s) in Google Scholar

Fasudil (HA-1077; AT877) Hydrochloride 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 is also a potent Ca²⁺ channel antagonist and vasodilator.

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Reinheit: 99.97%
CAS. Nr.: 105628-07-7
Formel: C₁₄H₁₈ClN₃O₂S
Molecular Weight:327.83

Speicherung:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

Fasudil Hydrochloride Chemical Structure

CAS. Nr.: 105628-07-7

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Use of MCE Products

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (29)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

p160ROCK

0.33 μM (Ki)

ROCK2

0.158 μM (IC₅₀)

PKA

4.58 μM (IC₅₀)

PKC

12.30 μM (IC₅₀)

PKG

1.65 μM (IC₅₀)

Alle ROCK Isoform-spezifische Produkte anzeigen :

Alle Calcium Channel Isoform-spezifische Produkte anzeigen :

Alle PKA Isoform-spezifische Produkte anzeigen :

Alle PKC Isoform-spezifische Produkte anzeigen :

Alle HIV Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
U-937	IC₅₀	35 μM Compound: HA-1077, Fasudil hydrochloride	Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay Inhibition of MCP1-induced cell migration in U937 cells expressing CCR2 by chemotaxis assay	[PMID: 17046269]

In Vitro

Fasudil Hydrochloride (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 (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 (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 24 hours
Incubation Time:

24 hours
Result:

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

In Vivo

Fasudil Hydrochloride (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 (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 (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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 105628-07-7
Appearance Solid
Molecular Weight 327.83
Formel C₁₄H₁₈ClN₃O₂S
Color White to off-white
SMILES

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

HA-1077 Hydrochloride; AT-877 Hydrochloride
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

* In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

Publications (29)

All WBIn Vivo Efficacy StudyCell Imaging/Staining

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Journal Impact Factor

Mol Cancer

ROCK1 inhibition primes anti-tumor immunity in EGFR-mutant NSCLC by triggering PD-L1 degradation mediated by SMURF2. [Abstract]

2026 Apr 2;25(1):130. PMID: 41928228
Nat Nanotechnol

Nanoparticles reach metastatic tumours via enhanced permeability of adjacent vessels. [Abstract]

2026 Jun;21(6):880-891. PMID: 42286217
Cell Mol Immunol

A SARS-CoV-2-specific CAR-T-cell model identifies felodipine, fasudil, imatinib, and caspofungin as potential treatments for lethal COVID-19. [Abstract]

2023 Apr;20(4):351-364. PMID: 36864189
Cell Stem Cell

Mechano-oncogenic cytoskeletal remodeling drives leukemic transformation with mitochondrial vesicle-mediated STING activation. [Abstract]

2025 Apr 3;32(4):581-597.e11. PMID: 39986274
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
NPJ Precis Oncol

GLMP promotes EGFR-TKI resistance by activating autophagy and RhoA pathway in non-small cell lung cancer. [Abstract]

2025 Nov 26;9(1):391. PMID: 41298761
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
Aging Cell

Hippocampal Nogo66-NgR1 signaling activation restricts postsynaptic assembly in aged mice with postoperative neurocognitive disorders. [Abstract]

2025 Jan;24(1):e14366. PMID: 39412367
Aging Cell

Sevoflurane-induced overexpression of extrasynaptic α5-GABAAR via the RhoA/ROCK2 pathway impairs cognitive function in aged mice. [Abstract]

2024 Jun 2:e14209. PMID: 38825816

Fasudil Hydrochloride purchased from MedChemExpress. Usage Cited in: Aging Cell. 2024 Jun 2:e14209. [Abstract]

Western blot images of ROCK2, radixin, and p-ERM bands in total protein samples and α5-GABAAR bands in membrane protein samples. β-Actin and NKA were used as total protein and membrane protein loading controls, respectively. Total proteins and membrane proteins were extracted from the mouse hippocampus. Aged C57BL/6 mice (female, 18–19 months old), Fasudil Hydrochloride (20 mg/kg/day; ip) for 7 days before anesthesia.

Fasudil Hydrochloride purchased from MedChemExpress. Usage Cited in: Aging Cell. 2024 Jun 2:e14209. [Abstract]

Escape latency in the training stage. Aged C57BL/6 mice (female, 18–19 months old), Fasudil Hydrochloride (20 mg/kg/day; ip) for 7 days before anesthesia.
Biochem Pharmacol

The dual targeting effects of KD025 on casein kinase 2 and ROCK2 in a mouse model of diet-induced obesity. [Abstract]

2025 Apr 8:116933. PMID: 40210126
Inflammopharmacology

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

2023 Aug;31(4):2037-2047. PMID: 37074600
Eur J Pharmacol

Fasudil attenuates oxidative stress-induced partial epithelial-mesenchymal transition of tubular epithelial cells in hyperuricemic nephropathy via activating Nrf2. [Abstract]

2024 May 13:975:176640. PMID: 38750716
Diabetol Metab Syndr

THBS1 regulates the function and insulin sensitivity of HTR8/SVneo cells treated with high glucose through the RhoA/ROCK1 signaling pathway. [Abstract]

2025 Oct 3;17(1):374. PMID: 41044623
Sci Rep

Anti-adipogenic effects of KD025 (SLx-2119), a ROCK2-specific inhibitor, in 3T3-L1 cells. [Abstract]

2018 Feb 6;8(1):2477. PMID: 29410516

Fasudil Hydrochloride purchased from MedChemExpress. Usage Cited in: Sci Rep. 2018 Feb 6;8(1):2477. [Abstract]

3T3-L1 cells were differentiated by incubation in DMI with KD025, Y-27632, or Fasudil Hydrochloride (fasudil; 10 μM) as indicated, and stained with Oil Red O on day 8.

Fasudil Hydrochloride purchased from MedChemExpress. Usage Cited in: Sci Rep. 2018 Feb 6;8(1):2477. [Abstract]

3T3-L1 pre-adipocytes were treated with KD025 (7 µM),Y-27632 (10µM), Fasudil Hydrochloride (fasudil ; 10 µM), H-1152P (3 µM), or SR3677 (5 µM) for one day.
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 Cereb Blood Flow Metab

Isoform-selective and non-selective rho-kinase inhibitors do not affect collagenase-induced intracerebral hemorrhage outcomes in mice: Influence of sex and circadian cycle. [Abstract]

2025 Jun;45(6):1191-1202. PMID: 39763388
iScience

A stress-responsive neurovascular axis shapes skin immune accessibility. [Abstract]

2026 Feb 23;29(3):115122. PMID: 41852725
Metab Brain Dis

Ginkgo biloba extract mediates HT22 cell proliferation and migration after oxygen-glucose deprivation/reoxygenation via regulating RhoA-ROCK2 signalling pathway. [Abstract]

2025 Jan 7;40(1):91. PMID: 39775993
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
Biomed Rep

Inhibiting Rho kinase 2 reduces memory dysfunction in adult rats exposed to sevoflurane at postnatal days 7-9. [Abstract]

2015 May;3(3):361-364. PMID: 26137236

Fasudil Hydrochloride purchased from MedChemExpress. Usage Cited in: Biomed Rep. 2015 May;3(3):361-364. [Abstract]

RhoA and ROCK2 upregulation in the rat hippocampus is involved in memory dysfunction induced by postnatal exposure of Sevoflurane. The expression of RhoA, ROCK2 and cleaved caspase-3 (Cl-Csp3) in the hippocampus of the S3 group significantly increased, compared to that of the C group (P<0.05). There is no difference of the level of RhoA, ROCK2 and Cl-Csp3 between the C and S1 groups (P>0.05). ROCK2 inhibitor Fasudil hydrochloride in the F group clearly decreases the expression of ROCK2 and Cl-Cs
Transl Neurosci

Hydrochloride fasudil attenuates brain injury in ICH rats. [Abstract]

2020 Apr 20;11(1):75-86. PMID: 33335751
Preprints

2025 Dec 2.
SSRN

2023 Feb 24.

Lösungsmittel & Löslichkeit

In Vitro:

H₂O : 55 mg/mL (167.77 mM; Need ultrasonic)

DMSO : ≥ 31 mg/mL (94.56 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.0504 mL

15.2518 mL

30.5036 mL

5 mM

0.6101 mL

3.0504 mL

6.1007 mL

10 mM

0.3050 mL

1.5252 mL

3.0504 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (6.34 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (6.34 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (6.34 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS

Solubility: 100 mg/mL (305.04 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact

MedChemExpress (MCE) .

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (286 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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)

Verweise

[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]. Corbin KD, et al. Choline metabolism provides novel insights into nonalcoholic fatty liver disease and its progression. Curr Opin Gastroenterol. 2012 Mar;28(2):159-65. [Content Brief]

[6]. 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]

[7]. 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]

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.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO / H₂O	1 mM	3.0504 mL	15.2518 mL	30.5036 mL	76.2590 mL
	5 mM	0.6101 mL	3.0504 mL	6.1007 mL	15.2518 mL
	10 mM	0.3050 mL	1.5252 mL	3.0504 mL	7.6259 mL
	15 mM	0.2034 mL	1.0168 mL	2.0336 mL	5.0839 mL
	20 mM	0.1525 mL	0.7626 mL	1.5252 mL	3.8130 mL
	25 mM	0.1220 mL	0.6101 mL	1.2201 mL	3.0504 mL
	30 mM	0.1017 mL	0.5084 mL	1.0168 mL	2.5420 mL
	40 mM	0.0763 mL	0.3813 mL	0.7626 mL	1.9065 mL
	50 mM	0.0610 mL	0.3050 mL	0.6101 mL	1.5252 mL
	60 mM	0.0508 mL	0.2542 mL	0.5084 mL	1.2710 mL
	80 mM	0.0381 mL	0.1906 mL	0.3813 mL	0.9532 mL
H₂O	100 mM	0.0305 mL	0.1525 mL	0.3050 mL	0.7626 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Fasudil Hydrochloride

29 Cited Publications

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Fasudil Hydrochloride

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Publications Citing Use of MedChemExpress (MCE) Fasudil Hydrochloride

Alle ROCK Isoform-spezifische Produkte anzeigen

Alle Calcium Channel Isoform-spezifische Produkte anzeigen

Alle PKA Isoform-spezifische Produkte anzeigen

Alle PKC Isoform-spezifische Produkte anzeigen

Alle HIV Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (29)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Fasudil Hydrochloride Related Classifications

HY-10341 Related Classifications