Chroman 1 [1273579-40-0]

Référence HY-15392-5mg

Conditionnement : 5mg

Marque : MedChemExpress


Description

Chroman 1 is a highly potent and selective ROCK inhibitor. Chroman 1 is more potent against ROCK2 (IC50=1 pM) than ROCK1 (IC50=52 pM). Chroman 1 also has inhibitory activity against MRCK, with an IC50 of 150 nM[1][2].

IC50 & Target[1][2]

ROCK2

1 pM (IC50)

ROCK1

52 pM (IC50)

MRCK

150 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
A7R5 IC50
< 4 nM
Compound: (S)-1
Inhibition of ROCK2-mediated myosin light chain bis-phosphorylation in rat A7r5 cells after 1 hr by TO-PRO-3 iodide staining-based assay
Inhibition of ROCK2-mediated myosin light chain bis-phosphorylation in rat A7r5 cells after 1 hr by TO-PRO-3 iodide staining-based assay
10.1039/C0MD00194E
In Vitro

Chroman 1 (50 nM, 24 h) inhibits caspase-3/7 activation and reduces apoptosis in human pluripotent stem cells[1].

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

Apoptosis Analysis[1]

Cell Line: hESCs (human pluripotent stem cells) (WA09)
Concentration: 50 nM
Incubation Time: 0-12 h or 24 h
Result: Reduced the number of apoptotic cells, reduced caspase-3/7 activation.

Western Blot Analysis[1]

Cell Line: hESCs (human pluripotent stem cells) (WA09)
Concentration: 50 nM
Incubation Time: 24 h
Result: Partially inhibited caspase-3 activation.
Masse moléculaire

436.50

Formule

C24H28N4O4

CAS No.
Appearance

Solid

Color

White to pink

SMILES

O=C([C@@H]1COC2=CC=C(OC)C=C2C1)NC3=CC=C(C4=CNN=C4)C=C3OCCN(C)C

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
Solvant et solubilité
In Vitro: 

DMSO : ≥ 50 mg/mL (114.55 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2910 mL 11.4548 mL 22.9095 mL
5 mM 0.4582 mL 2.2910 mL 4.5819 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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    90% Corn Oil

    Solubility: ≥ 3.25 mg/mL (7.45 mM); Clear solution

    This protocol yields a clear solution of ≥ 3.25 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 (32.5 mg/mL) to 900 μL Corn oil, and mix evenly.

  • Protocol 2

    Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

    Solubility: 2.5 mg/mL (5.73 mM); Suspended solution; Need ultrasonic

Pureté et documentation
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Prix HT
HY-10396-5mg
 5mg 
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 10mg 
HY-15392-1mL
 10mM/1mL