An inhibitor of PDE3
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Olprinone (hydrochloride)

Item No. 28396

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1,2-dihydro-5-imidazo[1,2-a]pyridin-6-yl-6-methyl-2-oxo-3-pyridinecarbonitrile, monohydrochloride
CAS Number
119615-63-3
Synonyms
  • Loprinone
Molecular Formula
C14H10N4O • HCl
Formula Weight
286.7
Purity
≥98%
Formulation
A crystalline solid
λmax
219, 262, 345 nm
SMILES
O=C1C(C#N)=CC(C2=CN3C(C=C2)=NC=C3)=C(C)N1.Cl
InChi Code
InChI=1S/C14H10N4O.ClH/c1-9-12(6-11(7-15)14(19)17-9)10-2-3-13-16-4-5-18(13)8-10;/h2-6,8H,1H3,(H,17,19);1H
InChi Key
PWTBMBAQRAOAFF-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Cayman Chemical
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    Product Description

    Olprinone is an inhibitor of phosphodiesterase 3 (PDE3; IC50 = 0.35 μM for human cardiac enzyme).1 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).2 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.3 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.4 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.5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Sugioka, M., Masuoka, H., Ichikawa, K., et al. Identification and characterization of isoenzymes of cyclic nucleotide phosphodiesterase in human kidney and heart, and the effects of new cardiotonic agents on these isoenzymes. Naunyn. Schmiedebergs. Arch. Pharmacol. 350(3), 284-293 (1994).

    2. Minonishi, T., Ogawa, K., Tokinaga, Y., et al. Differential vasodilation response to olprinone in rabbit renal and common carotid arteries. J. Anesth. 24(1), 61-66 (2010).

    3. Han, M.-X., Xu, X.-W., Lu, S.-Q., et al. Effect of olprinone on ischemia-reperfusion induced myocardial injury in rats. Biomed. Pharmacother. 111, 1005-1012 (2019).

    4. Genovese, T., Mazzon, E., Paterniti, I., et al. Neuroprotective effects of olprinone after cerebral ischemia/reperfusion injury in rats. Neurosci. Lett. 503(2), 93-99 (2011).

    5. Koike, T., Nadeen Qutab, M., Tsuchida, M., et al. Pretreatment with olprinone hydrochloride, a phosphodiesterase III inhibitor, attenuates lipopolysaccharide-induced lung injury via an anti-inflammatory effect. Pulm. Pharmacol. 21(1), 166-171 (2008).