1. Cell Cycle/DNA Damage
    TGF-beta/Smad
    Stem Cell/Wnt
  2. ROCK
  3. Hydroxyfasudil

Hydroxyfasudil (Synonyms: HA-1100)

Cat. No.: HY-13911 Purity: 98.11%
Handling Instructions

Hydroxyfasudil is a ROCK inhibitor, with IC50s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively.

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

Hydroxyfasudil Chemical Structure

Hydroxyfasudil Chemical Structure

CAS No. : 105628-72-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 123 In-stock
Estimated Time of Arrival: December 31
5 mg USD 112 In-stock
Estimated Time of Arrival: December 31
10 mg USD 136 In-stock
Estimated Time of Arrival: December 31
50 mg USD 594 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Hydroxyfasudil:

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Description

Hydroxyfasudil is a ROCK inhibitor, with IC50s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively.

IC50 & Target[1]

ROCK2

0.72 μM (IC50)

ROCK1

0.73 μM (IC50)

PKA

37 μM (IC50)

In Vitro

Hydroxyfasudil is a ROCK inhibitor, with IC50s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively. Hydroxyfasudil also less potently inhibits PKA, with an IC50 of 37 μM, 50-fold higher than those of the ROCKs. Hydroxyfasudil increases eNOS mRNA levels, with an EC50 value of 0.8 ± 0.3 μM. Hydroxyfasudil (0-100 μM) concentration-dependently increases eNOS activity and stimulates NO production in human aortic endothelial cells (HAEC). Hydroxyfasudil (10 μM) increases the half-life of eNOS mRNA from 13 to 16 hours, but does not affect eNOS promoter activity at concentrations from 0.1 to 100 μM[1].

In Vivo

Hydroxyfasudil (10 mg/kg, i.p.) significantly increases both the average and maximal voided volumes in SD rats. Hydroxyfasudil also significantly decreases the maximal detrusor pressure[2]. Hydroxyfasudil (3 mg/kg, i.p) inhibits hypercontractility induced by norepinephrine in spontaneously hypertensive rats (SHRs). Furthermore, Hydroxyfasudil (3, 10 mg/kg, i.p) significantly ameliorates decreased penile cGMP contents in rats[3].

Molecular Weight

307.37

Formula

C₁₄H₁₇N₃O₃S

CAS No.

105628-72-6

SMILES

O=C1NC=CC2=C1C=CC=C2S(=O)(N3CCNCCC3)=O

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 31 mg/mL (100.86 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2534 mL 16.2670 mL 32.5341 mL
5 mM 0.6507 mL 3.2534 mL 6.5068 mL
10 mM 0.3253 mL 1.6267 mL 3.2534 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 0.5 mg/mL (1.63 mM); Clear solution

  • 2.

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

    Solubility: ≥ 0.5 mg/mL (1.63 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 0.5 mg/mL (1.63 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[2]

Micturition behavior is studied after intraperitoneal injection of either Hydroxyfasudil (10 mg/kg) or a corresponding volume of saline. Each rat is placed in a metabolic cage containing a urine collection funnel that is placed over an electronic balance. The balance is connected to a personal computer via a multiport controller and used to measure the cumulative weight of the collected urine. Every 150 s during a continuous 24-h period, the computer samples and records the data for the micturition frequency and volumes. The micturition reflex parameters that are collected includ: urine volume per micturition, maximal micturition volume, micturition frequency, and total urine output in the Hydroxyfasudil- or vehicle-treated animals. Each monitoring session started at 18.00 hours. Prior to being placed in the metabolic cage at the start of each experimental period, the animals receive either a single injection of Hydroxyfasudil (10 mg/kg) dissolved in saline or an injection of saline without the inhibitor[2].

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

References

Purity: 98.11%

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Hydroxyfasudil
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