Rho-Kinase-IN-2 (Compound 23) 是一种具有口服活性的、选择性的和中枢神经系统 (CNS) 渗透性的 Rho激酶 (ROCK) 抑制剂 (ROCK2 IC₅₀=3 nM)。Rho-Kinase-IN-2 可用于亨廷顿病的研究。

Rho-Kinase-IN-2 (Compound 23) is an orally active, selective, and central nervous system (CNS)-penetrant Rho Kinase (ROCK) inhibitor (ROCK2 IC 50 =3 nM). Rho-Kinase-IN-2 can be used in Huntington’s research.

Solid

ROCK2 3 nM (IC50)

Rho-Kinase-IN-2 (0-10 mM, 1 hour) treatment shows an increase in AKT phosphorylation and a decrease in MYPT1 phosphorylation. has not independently confirmed the accuracy of these methods. They are for reference only.Western Blot Analysis

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.
Rho-Kinase-IN-2 (oral adiministration; 10 or 20 mg/kg; QD or BID; 2 weeks) treatment shows excellent tolerability assessment.
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.
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.
Rho-Kinase-IN-2 (oral adiministration; 10 mg/kg; twice a day; 90 days) treatment leads to lower-than-expected brain concentrations. has not independently confirmed the accuracy of these methods.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Tammy Ladduwahetty, et al. Identification of a Potent, Selective, and Brain-Penetrant Rho Kinase Inhibitor and its Activity in a Mouse Model of Huntingtons Disease. J Med Chem. 2022 Jul 11.

In Vitro: DMSO : 50 mg/mL (134.25 mM; Need ultrasonic)配制储备液