An inhibitor of PDE3 (IC50 = 0.35 μM for human cardiac enzyme); selective for PDE3 over PDE1 and PDE2 (IC50s = 150 and 100 μM

Olprinone (hydrochloride) – 1 mg

Brand:
Cayman
CAS:
119615-63-3
Storage:
-20
UN-No:
Non-Hazardous - /

Olprinone is an inhibitor of phosphodiesterase 3 (PDE3; IC50 = 0.35 μM for human cardiac enzyme).{51184} It is selective for PDE3 over PDE1 and PDE2 (IC50s = 150 and 100 μM, respectively). Olprinone induces relaxation of precontracted isolated rabbit renal and carotid arterial rings (IC50s = 40 and 103 nM, respectively).{51185} It reduces infarct size and improves cardiac function in a rat model of myocardial ischemia-reperfusion injury when administered at a dose of 0.6 mg/kg twice per day.{51186} Olprinone (0.2 mg/kg) reduces cortical and striatal damage, as well as reduces injured cerebral tissue nitrotyrosine formation, apoptosis, and levels of inducible nitric oxide synthase (iNOS), IL-1β, and intercellular adhesion molecule 1 (ICAM-1) in a rat model of cerebral ischemia-reperfusion injury.{51187} It inhibits neutrophil infiltration into the lungs and inhibits increases in serum levels of TNF-α and IL-6 in a rat model of LPS-induced lung inflammation when administered at a dose of 0.2 mg/kg.{51188}  

 

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Description

An inhibitor of PDE3 (IC50 = 0.35 μM for human cardiac enzyme); selective for PDE3 over PDE1 and PDE2 (IC50s = 150 and 100 μM, respectively); induces relaxation of precontracted isolated rabbit renal and carotid arterial rings (IC50s = 40 and 103 nM, respectively); reduces infarct size and improves cardiac function in a rat model of myocardial ischemia-reperfusion injury at 0.6 mg/kg twice per day; reduces cortical and striatal damage, as well as reduces injured cerebral tissue nitrotyrosine formation, apoptosis, and levels of iNOS, IL-1β, and ICAM-1 in a rat model of cerebral ischemia-reperfusion injury at 0.2 mg/kg; inhibits neutrophil infiltration into lung and inhibits increases in serum levels of TNF-α and IL-6 in a rat model of LPS-induced lung inflammation at 0.2 mg/kg

Formal name: 1,2-dihydro-5-imidazo[1,2-a]pyridin-6-yl-6-methyl-2-oxo-3-pyridinecarbonitrile, monohydrochloride

Synonyms:  Loprinone

Molecular weight: 286.7

CAS: 119615-63-3

Purity: ≥98%

Formulation: A crystalline solid

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