1. Membrane Transporter/Ion Channel
    Metabolic Enzyme/Protease
  2. Potassium Channel
    Phosphodiesterase (PDE)
    Drug Metabolite
  3. OR-1896

OR-1896 

Cat. No.: HY-135746 Purity: 98.90%
Handling Instructions

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.

For research use only. We do not sell to patients.

OR-1896 Chemical Structure

OR-1896 Chemical Structure

CAS No. : 220246-81-1

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Description

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[1].

IC50 & Target[1]

PDE3/PDE Ⅲ

 

K+ Channel

 

Drug Metabolite

 

In Vitro

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[1].

In Vivo

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[1].

Molecular Weight

245.28

Formula

C₁₃H₁₅N₃O₂

CAS No.

220246-81-1

SMILES

CC(NC1=CC=C(C([[email protected]](C)C2)=NNC2=O)C=C1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
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Keywords:

OR-1896OR1896OR 1896Potassium ChannelPhosphodiesterase (PDE)Drug MetaboliteKcsALevosimendanmetabolismcardioprotectionPDE-IIIATP-sensitiveK+-channelsCa2+-sensitizingvasodilatorylong-livedInhibitorinhibitorinhibit

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OR-1896
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HY-135746
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