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    TGF-beta/Smad
  2. ROCK
  3. Rho-Kinase-IN-2

Rho-Kinase-IN-2 

Cat. No.: HY-150640
Handling Instructions

Rho-Kinase-IN-2 (Compound 23) is an orally active, selective, and central nervous system (CNS)-penetrant Rho Kinase (ROCK) inhibitor (ROCK2 IC50=3 nM). Rho-Kinase-IN-2 can be used in Huntington’s research.

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

Rho-Kinase-IN-2 Chemical Structure

Rho-Kinase-IN-2 Chemical Structure

CAS No. : 2573071-18-6

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Description

Rho-Kinase-IN-2 (Compound 23) is an orally active, selective, and central nervous system (CNS)-penetrant Rho Kinase (ROCK) inhibitor (ROCK2 IC50=3 nM). Rho-Kinase-IN-2 can be used in Huntington’s research[1].

IC50 & Target

ROCK2

3 nM (IC50)

In Vitro

Rho-Kinase-IN-2 (0-10 mM, 1 hour) treatment shows an increase in AKT phosphorylation and a decrease in MYPT1 phosphorylation[1].

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

Western Blot Analysis[1]

Cell Line: A7r5 and PANC1 cells
Concentration: 0-10 mM
Incubation Time: 1 hour
Result: Showed concentration-dependent effects, leading to an increase in AKT phosphorylation (EC50=28 nM) and a decrease in MYPT1 phosphorylation (IC50=14 nM).
In Vivo

Rho-Kinase-IN-2 (oral adiministration; 10 mg/kg; 6 times; 0.5, 1, 2, 4, 8, and 12 h) treatment shows dose- and time-dependent ROCK1 and ROCK2 target engagement[1].
Rho-Kinase-IN-2 (oral adiministration; 10 or 20 mg/kg; QD or BID; 2 weeks) treatment shows excellent tolerability assessment[1].
Rho-Kinase-IN-2 (oral adiministration; 1-20 mg/kg; once) treatment shows a direct dose- and time-dependent relationship between brain exposure and MYPT1 phosphorylation status[1].
Rho-Kinase-IN-2 (oral adiministration; 10 or 20 mg/kg; once) treatment decreases in the mean arterial, systolic, diastolic blood pressure, and heart rate[1].
Rho-Kinase-IN-2 (oral adiministration; 10 mg/kg; twice a day; 90 days) treatment leads to lower-than-expected brain concentrations[1].

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

Animal Model: Male C57BL/6 mice[1]
Dosage: 10 mg/kg
Administration: Oral adiministration; 10 mg/kg; 6 times; 0.5, 1, 2, 4, 8, and 12 h
Result: Observed dose- and time-dependent ROCK1 and ROCK2 TE, with a free brain KiNativ ROCK1 and ROCK2 IC50=∼6 nM.
Animal Model: 3−4 months old heterozygote Q175DN KI and wild-type littermate mice[1]
Dosage: 10 or 20 mg/kg
Administration: Oral adiministration; 10 or 20 mg/kg; once a day or twice a day; 2 weeks
Result: Scored neurological index normally at all doses although a slight loss in bodyweight (∼2%) in the 20 mg/kg treatment group.
Animal Model: Heterozygote HTT zQ175DN knock-in mice[1]
Dosage: 1-20 mg/kg
Administration: Oral adiministration; 1-20 mg/kg; once
Result: Remained over MYPT1 IC50 for over 2 h of the free brain at 10 mg/kg, and observed the dose- and time-dependent inhibition of MYPT1 phosphorylation in the striatum following acute in vivo dosing.
Animal Model: CD1 mice[1]
Dosage: 10 and 20 mg/kg
Administration: Oral adiministration; 10 or 20 mg/kg; once
Result: Observed the decreases in the mean arterial (maximum change of 61.0 ± 8.5 mmHg from baseline), systolic (maximum change of 59.5 ± 8.4 mmHg from baseline), diastolic blood pressure (maximum change of 56.4 ± 9.0 mmHg from baseline), and heart rate (maximum change from predose of 107 bpm) when compared to the control group from ∼0.5 to 2 h post dose.
Animal Model: Heterozygote Q175DN KI mouse model of HD[1]
Dosage: 10 mg/kg
Administration: Oral adiministration; 10 mg/kg; twice a day; 90 days
Result: Led to lower-than-expected brain concentrations compared to single dosing.
Molecular Weight

372.44

Formula

C20H25FN4O2

CAS No.
SMILES

O=C(N1[[email protected]](C)CN(C2=C(F)C=NC=C2)CC1)N[[email protected]@H](C3=CC=CC(OC)=C3)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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