OR-1896

Research use only, not for human use.

OR-1896 is the active metabolite of Levosimendan, a highly specific phosphodiesterase (PDE III) inhibitor, a vasodilator with partial anti-inflammatory properties that produces vasodilation in different types of blood vessels through activation of ATP-sensitive (KATP) and other potassium channels.

OR-1896 is an active long-lived metabolite of Levosimendan. OR-1896 is a highly selective phosphodiesterase (PDE) III isoform inhibitor and a powerful vasodilator. OR-1896 can open ATP-sensitive K+ channels and has Ca2+-sensitizing effect. OR-1896 mitigates cardiomyocyte apoptosis, cardiac remodeling and myocardial inflammation.

There are many evidences has accumulated and revealed a variety of beneficial pleiotropic effects OR-1896. OR-1896 evokes prominent vasodilatory responses, activation of ATP-sensitive sarcolemmal K+ channels of smooth muscle cells appears as a powerful vasodilator mechanism. Additionally, activation of ATP-sensitive K+ channels in the mitochondria potentially extends the range of cellular actions towards the modulation of mitochondrial ATP production and implicates a pharmacological mechanism for cardioprotection.

During the metabolism of Levosimendan approximately 5% of the drug is converted to the metabolite OR-1855 in the large intestine, and then acetylated in the liver to form the active metabolite OR-1896. Binding to plasma proteins is 98% for Levosimendan but only 40% for OR-1896. Unlike Levosimendan, which has an elimination half-life of 1-1.5 h, the half-life of OR-1896 is about 75 to 80 h allowing cardiovascular effects to persist up to 7 to 9 days after discontinuation of a 24-hour infusion of levosimendan. The pharmacokinetic of the parent drug is unaltered in subjects with severe renal impairment or with moderate hepatic impairment, whereas the elimination of its metabolites (OR-1896) can be prolonged.

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Cell Cycle/DNA Damage

Potassium Channel

Potassium Channel | PDE

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220246-81-1

245.28

C13H15N3O2

>98% (HPLC)

In Vitro:?DMSO : 62.5 mg/mL (254.81 mM; Ultrasonic )

C[C@@H]1CC(=O)NN=C1c1ccc(NC(C)=O)cc1

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(-20℃)

With Ice Pack

≥ 2 years