Product Name :
OR-1896
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.
CAS:
220246-81-1
Molecular Weight:
245.28
Formula:
C13H15N3O2
Chemical Name:
N-4-[(4R)-4-methyl-6-oxo-1, 4, 5, 6-tetrahydropyridazin-3-yl]phenylacetamide
Smiles :
CC(=O)NC1C=CC(=CC=1)C1=NNC(=O)C[C@H]1C
InChiKey:
GDZXNMWZXLDEKG-MRVPVSSYSA-N
InChi :
InChI=1S/C13H15N3O2/c1-8-7-12(18)15-16-13(8)10-3-5-11(6-4-10)14-9(2)17/h3-6,8H,7H2,1-2H3,(H,14,17)(H,15,18)/t8-/m1/s1
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥360 days if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
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.|Product information|CAS Number: 220246-81-1|Molecular Weight: 245.28|Formula: C13H15N3O2|Chemical Name: N-4-[(4R)-4-methyl-6-oxo-1, 4, 5, 6-tetrahydropyridazin-3-yl]phenylacetamide|Smiles: CC(=O)NC1C=CC(=CC=1)C1=NNC(=O)C[C@H]1C|InChiKey: GDZXNMWZXLDEKG-MRVPVSSYSA-N|InChi: InChI=1S/C13H15N3O2/c1-8-7-12(18)15-16-13(8)10-3-5-11(6-4-10)14-9(2)17/h3-6,8H,7H2,1-2H3,(H,14,17)(H,15,18)/t8-/m1/s1|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : 62.5 mg/mL (254.81 mM; Need ultrasonic)|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥360 days if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|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.Pozelimab Immunology/Inflammation |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.Gemtuzumab manufacturer Binding to plasma proteins is 98% for Levosimendan but only 40% for OR-1896.PMID:32686498 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.|References:|Papp, Z, et al., Levosimendan: molecular mechanisms and clinical implications: consensus of experts on the mechanisms of action of levosimendan. Int J Cardiol. 2012 Aug 23;159(2):82-7.Products are for research use only. Not for human use.|