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> Y-27632 (dihydrochloride) [129830-38-2]

Y-27632 (dihydrochloride) [129830-38-2]

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Référence HY-10583-50mg

Conditionnement : 50mg

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Description

Y-27632 dihydrochloride is an orally active and ATP-competitive ROCK (Rho-kinase) inhibitor (ROCK-I Ki=220 nM; ROCK-II Ki=300 nM). Y-27632 dihydrochloride shows antiepileptic effects[1][2][3][4].

IC50 & Target[1]

ROCK-I

220 nM (Ki)

ROCK-II

300 nM (Ki)

PKN

3.1 μM (Ki)

Citron kinase

5.3 μM (Ki)

PKCα

73 μM (Ki)

PKA

25 μM (Ki)

In Vitro

Y-27632 (1-5 μM; 0-60 min) promotes neuronal differentiation of adipose tissue-derived stem cells (ADSCs) [3].
Y-27632 (1-5 μM; 0-60 min) induces the expression of NSE, MAP-2 and nestin in ADSCs [3].

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

Y-27632 dihydrochloride Related Antibodies

Western Blot Analysis[3]

Cell Line: Adipose tissue-derived stem cells (ADSCs)
Concentration: 20 μM
Incubation Time: 24 hours
Result: Resulted in the up-regulation of NSE, MAP-2 and nestin protein levels by 25.3, 3.1 and 2.5 fold, respectively, compared to control cells not treated by Y-27632.
In Vivo

Y-27632 (oral gavage; 30 mg/kg; once daily; 4 w) prevents dimethylnitrosamine-induced hepatic fibrosis in rats[1].
Y-27632 (oral gavage; 5-10 mg/kg; once) shows antiepileptic effects in epilepsy induced by PTZ and MES[2].

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

Animal Model: Male Wistar rats injected with dimethylnitrosamine[1]
Dosage: 30 mg/kg
Administration: Oral gavage; 30 mg/kg; once daily; 4 weeks
Result: Decreased the occurrence of dimethylnitrosamine-induced hepatic fibrosis and reduced the collagen and hydroxyproline content and α-smooth muscle actin expression in the liver.
Animal Model: Male Swiss albino mice injected with PTZ (pentylenetetrazole) or induced by MES (maximal electroconvulsive shock)[2]
Dosage: 5-10 mg/kg
Administration: Oral gavage; 5-10 mg/kg; once
Result: Prolonged the onset time of myoclonic jerks when compared with those observed in the saline group (P<0.05).
Prolonged the onset time of clonic convulsions when compared with saline group (P<0.05).
Prevented the occurrence of tonic hindlimb extensions and death.
Masse moléculaire

320.26

Formule

C14H23Cl2N3O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C([C@@H]1CC[C@]([C@H](N)C)(05)CC1)NC2=CC=NC=C2.05Cl.05Cl
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, sealed storage, away from moisture

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

Solvant et solubilité
In Vitro: 

H2O : 100 mg/mL (312.25 mM; Need ultrasonic)

DMSO : 50 mg/mL (156.12 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 3.1225 mL 15.6123 mL 31.2246 mL
5 mM 0.6245 mL 3.1225 mL 6.2449 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* 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.

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: ≥ 2.5 mg/mL (7.81 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (7.81 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

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: 220 mg/mL (686.94 mM); Clear solution; Need ultrasonic

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.
Calculation results:
Working solution concentration: 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).
Pureté et documentation
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