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Hydroxyfasudil

Name: Hydroxyfasudil
Brand: TargetMol
SKU: T4276L
Price: 34 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T4276LCas No. 105628-72-6

Alias Hydroxy-Fasudil, HA-1100

Hydroxyfasudil (Hydroxy-Fasudil) is a ROCK inhibitor(IC50s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively).

Hydroxyfasudil

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Purity: 98.13%

Catalog No. T4276LAlias Hydroxy-Fasudil, HA-1100Cas No. 105628-72-6

Hydroxyfasudil (Hydroxy-Fasudil) is a ROCK inhibitor(IC50s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively).

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$34	In Stock	In Stock
10 mg	$51	In Stock	In Stock
25 mg	$95	In Stock	In Stock
50 mg	$155	In Stock	In Stock
100 mg	$245	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$37	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:98.13%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

Hydroxyfasudil AI Summary

Hydroxyfasudil is a multifaceted inhibitor with significant bioactivity against various enzymes and possesses antiviral properties. It exhibits notable selectivity for ROCK1 over PKA, with a Ki of 150.0 nM against ROCK1 and 2200.0 nM against PKA, resulting in a selectivity ratio of 15.0. Additionally, it inhibits human ROCK1 and ROCK2 with IC50 values of 758.58 nM and 575.44 nM, respectively, and demonstrates inhibition of ROCK-1 with a Ki value of 31.62 nM. Beyond its activity on ROCK enzymes, Hydroxyfasudil also inhibits Cruzain (4466.8 nM), Aldehyde Dehydrogenase 1 (ALDH1A1) (23755.8 nM), and HPGD (15-Hydroxyprostaglandin Dehydrogenase) (14125.4 nM). It further shows activity against human ERG with a Ki of 7943.28 nM and reduces MCP1-mediated human THP cell migration with an IC50 of 6918.31 nM. The compound demonstrates oral bioavailability in C57 mice at 57.0%, a clearance rate of 34.0 mL.min-1.kg-1, volume of distribution at steady state of 2.4 L.kg-1, and a half-life of 0.75 hours. Additionally, it shows good kinetic solubility in pH 7.4 PBS buffer (> 200000.0 nM) and a logP value of 1.43. In terms of antiviral activity, Hydroxyfasudil inhibits SARS-CoV-2 induced cytotoxicity in Caco-2 cells at a concentration of 10 µM with an inhibition rate of 7.36% and shows efficacy against the SARS-CoV-2 3CL-Pro protease at 20 µM with inhibition rates of 18.62% and 8.854%. It also has measurable inhibition against HDAC6, with percentages of 9.53% and 8.82% using different substrates. Lastly, it demonstrates inhibition of PARP1 with an IC50 value of 27,000.0 nM and has shown antiinvasive activity in human HT1080 cells at 50 µM with an activity of 50.0%..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Hydroxyfasudil (Hydroxy-Fasudil) is a ROCK inhibitor(IC50s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively).
Targets&IC50	ROCK2:0.72 μM, ROCK1:0.73 μM, PKA:37 μM
Synonyms	Hydroxy-Fasudil, HA-1100

Chemical Properties

Molecular Weight	307.37
Formula	C₁₄H₁₇N₃O₃S
Cas No.	105628-72-6
Smiles	O=c1[nH]ccc2c(cccc12)S(=O)(=O)N1CCCNCC1
Relative Density.	1.329g/cm3

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 31 mg/mL (100.86 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 0.5 mg/mL (1.63 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.2534 mL	16.2670 mL	32.5341 mL	162.6704 mL
5 mM	0.6507 mL	3.2534 mL	6.5068 mL	32.5341 mL
10 mM	0.3253 mL	1.6267 mL	3.2534 mL	16.2670 mL
20 mM	0.1627 mL	0.8134 mL	1.6267 mL	8.1335 mL
50 mM	0.0651 mL	0.3253 mL	0.6507 mL	3.2534 mL
100 mM	0.0325 mL	0.1627 mL	0.3253 mL	1.6267 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc