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CAS No. : 2573071-18-6
MCE 国际站:Rho-Kinase-IN-2
产品活性: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。
研究领域:Cell Cycle/DNA Damage | Stem Cell/Wnt | Cytoskeleton | TGF-beta/Smad
作用靶点:ROCK
In Vitro: Rho-Kinase-IN-2 (0-10 mM, 1 hour) treatment shows an increase in AKT phosphorylation and a decrease in MYPT1 phosphorylation.
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.
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.
相关产品:Bioactive Compound Library Plus | Cell Cycle/DNA Damage Compound Library | Kinase Inhibitor Library | Stem Cell Signaling Compound Library | TGF-beta/Smad Compound Library | CNS-Penetrant Compound Library | Anti-Aging Compound Library | Reprogramming Compound Library | Cytoskeleton Compound Library | Orally Active Compound Library | Anti-Pulmonary Fibrosis Compound Library | Cancer Stem Cells Compound Library | Heterocyclic Compound Library | Membrane Protein-targeted Compound Library | Highly Selective Inhibitors Library | Chroman 1 dihydrochloride | Ripasudil free base | AS1892802 | Hu7691 free base | Sovesudil | AT13148 | CRT0066854 | LX7101 | Y-27632 dihydrochloride | RKI-1447 | HA-100 hydrochloride | WF-536 | Pentanoic acid-d9 | Fasudil dihydrochloride | ROCK-IN-5 | ROCK2-IN-5 | BDP5290 | PF-4950834 | PT-262 | Afuresertib hydrochloride | Belumosudil mesylate | GSK429286A | Y-27632 dihydrochloride (GMP) | H-1152 dihydrochloride | 3-(4-Pyridyl)indole | ROCK inhibitor-2 | ROCK-IN-7 | ZINC00881524
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