Description
A ROCK inhibitor (IC50s = 5.6 and 6 nM for ROCK-I and ROCK-II, respectively); selective for ROCK-I and ROCK-II over Akt1, Akt2, and Akt3 (IC50s = 324, 1,950, and 1,290 nM, respectively), as well as Cdk2, GSK3α, IKKβ, JNK3, and Plk (IC50s = ≥7,000 nM for all), but also inhibits RSK1 and MSK1 (IC50s = 35 and 14 nM, respectively); inhibits LPS-induced TNF-α and IL-6 production in THP-1 cells; induces relaxation of pre-contracted isolated rat aortic rings (IC50 = 39 nM); reduces blood pressure in spontaneously hypertensive rats in a dose-dependent manner and in DOCA-salt hypertensive rats at 1 mg/kg; reduces pulmonary and systemic arterial pressure and increases cardiac output in normotensive rats and rats with monocrotaline-induced pulmonary hypertension at 30, 100, and 300 μg/kg, i.v.
Formal name: [2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-1H-imidazo[4,5-c]pyridin-7-yl][(3S)-3-amino-1-pyrrolidinyl]-methanone, dihydrochloride
Synonyms:
Molecular weight: 415.3
CAS: 607373-46-6
Purity: ≥98%
Formulation: A solid
