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> ROCK inhibitor-2 [1127308-52-4]

ROCK inhibitor-2 [1127308-52-4]

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Referencia HY-119937-1ml

embalaje : 10mM/1mL

Marca : MedChemExpress

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ROCK inhibitor-2 (compound 6) is a selective dual inhibitor of ROCK1 and ROCK2, with IC50 values of 160 nM and 21 nM, respectively. ROCK inhibitor-2 inhibits pMYPT1 with IC50 of 75 nM.

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ROCK inhibitor-2 Estructura química

ROCK inhibitor-2 Estructura química

No. CAS : 1127308-52-4

This product is a controlled substance and not for sale in your territory.

Based on 2 publication(s) in Google Scholar

Ver todos los productos específicos de isoformas ROCK:

Ver todas las isoformas
ROCK ROCK1 ROCK2
Descripciòn

ROCK inhibitor-2 (compound 6) is a selective dual inhibitor of ROCK1 and ROCK2, with IC50 values of 160 nM and 21 nM, respectively. ROCK inhibitor-2 inhibits pMYPT1 with IC50 of 75 nM[1].

IC50 & Target[1]

ROCK1

160 nM (IC50)

ROCK2

21 nM (IC50)

Peso molecular

332.40

Fòrmula

C21H20N2O2
No. CAS

1127308-52-4

Appearance

Solid

Color

White to light yellow

SMILES

O=C(N[C@H](C)C1=CC=CC(OC)=C1)C(C=C2)=CC=C2C3=CC=NC=C3
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvente y solubilidad
In Vitro: 

DMSO : 200 mg/mL (601.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0084 mL 15.0421 mL 30.0842 mL
5 mM 0.6017 mL 3.0084 mL 6.0168 mL
View the Complete Stock Solution Preparation Table

* 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Calculadora de molaridad

  • Calculadora de dilución

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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: ≥ 5 mg/mL (15.04 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 5 mg/mL (15.04 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación

Purity: 99.92%

SDS (251 KB)

COA (245 KB) HNMR (259 KB) RP-HPLC (159 KB) LCMS (374 KB)

Instrucciones de manejo (2659 KB)
Referencias

  • [1]. Hobson AD, et al. Identification of Selective Dual ROCK1 and ROCK2 Inhibitors Using Structure-Based DrugDesign. J Med Chem. 2018 Dec 27;61(24):11074-11100.  [Content Brief]

  • [1]. Hobson AD, et al. Identification of Selective Dual ROCK1 and ROCK2 Inhibitors Using Structure-Based DrugDesign. J Med Chem. 2018 Dec 27;61(24):11074-11100.

Complete Stock Solution Preparation Table

* 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0084 mL 15.0421 mL 30.0842 mL 75.2106 mL
5 mM 0.6017 mL 3.0084 mL 6.0168 mL 15.0421 mL
10 mM 0.3008 mL 1.5042 mL 3.0084 mL 7.5211 mL
15 mM 0.2006 mL 1.0028 mL 2.0056 mL 5.0140 mL
20 mM 0.1504 mL 0.7521 mL 1.5042 mL 3.7605 mL
25 mM 0.1203 mL 0.6017 mL 1.2034 mL 3.0084 mL
30 mM 0.1003 mL 0.5014 mL 1.0028 mL 2.5070 mL
40 mM 0.0752 mL 0.3761 mL 0.7521 mL 1.8803 mL
50 mM 0.0602 mL 0.3008 mL 0.6017 mL 1.5042 mL
60 mM 0.0501 mL 0.2507 mL 0.5014 mL 1.2535 mL
80 mM 0.0376 mL 0.1880 mL 0.3761 mL 0.9401 mL
100 mM 0.0301 mL 0.1504 mL 0.3008 mL 0.7521 mL
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ROCK inhibitor-2 Related Classifications

  • Cell Cycle/DNA Damage TGF-beta/Smad Stem Cell/Wnt Cytoskeleton
  • ROCK
Help & FAQs

Keywords:

ROCK inhibitor-21127308-52-4ROCK inhibitor2ROCK inhibitor 2ROCKRho-associated protein kinaseRho-associated kinaseRho-kinaseROKpMYPT1Inhibitorinhibitorinhibit

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