製品番号: HY-135746

OR-1896

2 Cited Publications

カスタマーレビュー

Based on 2 publication(s) in Google Scholar

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.

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純度: 99.04%
CAS 番号: 220246-81-1
分子式: C₁₃H₁₅N₃O₂
分子量:245.28

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

OR-1896 構造式

CAS 番号: 220246-81-1

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
化学情報
Publications (2)
溶剤 & 溶解度
- 体外
- 体内
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target^[1]

PDE3/PDE Ⅲ

K+ Channel

Drug Metabolite

Phosphodiesterase (PDE) アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	EC₅₀	>1000 nM Compound: 2	Cytotoxicity against human HeLa cells assessed as cell growth inhibition measured after 48 hrs by Caspase-Glo reagent based assay Cytotoxicity against human HeLa cells assessed as cell growth inhibition measured after 48 hrs by Caspase-Glo reagent based assay	[PMID: 31749907]

体外実験

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

体内実験

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

化学情報

CAS 番号 220246-81-1
性状 Solid
分子量 245.28
分子式 C₁₃H₁₅N₃O₂
Color Light yellow to yellow
SMILES

CC(NC1=CC=C(C([C@H](C)C2)=NNC2=O)C=C1)=O
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (2)

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Pharmaceuticals (Basel)

Monitoring of Levosimendan Administration in Patients with Pulmonary Hypertension Undergoing Cardiac Surgery and Effect of Two Different Dosing Schemes on Hemodynamic and Echocardiographic Parameters. [Abstract]

2023 May 30;16(6):815. PMID: 37375762
J Pharm Biomed Anal

Highly sensitive ultra-high-performance liquid chromatography coupled with tandem mass spectrometry method for the multiplex analysis of levosimendan and its metabolites OR-1855 and OR-1896 in human plasma. [Abstract]

2025 Mar 15:255:116612. PMID: 39721342

溶剤 & 溶解度

体外:

DMSO : 62.5 mg/mL (254.81 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

4.0770 mL

20.3849 mL

40.7697 mL

5 mM

0.8154 mL

4.0770 mL

8.1539 mL

10 mM

0.4077 mL

2.0385 mL

4.0770 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (8.48 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (8.48 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (8.48 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (274 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. 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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	4.0770 mL	20.3849 mL	40.7697 mL	101.9243 mL
	5 mM	0.8154 mL	4.0770 mL	8.1539 mL	20.3849 mL
	10 mM	0.4077 mL	2.0385 mL	4.0770 mL	10.1924 mL
	15 mM	0.2718 mL	1.3590 mL	2.7180 mL	6.7950 mL
	20 mM	0.2038 mL	1.0192 mL	2.0385 mL	5.0962 mL
	25 mM	0.1631 mL	0.8154 mL	1.6308 mL	4.0770 mL
	30 mM	0.1359 mL	0.6795 mL	1.3590 mL	3.3975 mL
	40 mM	0.1019 mL	0.5096 mL	1.0192 mL	2.5481 mL
	50 mM	0.0815 mL	0.4077 mL	0.8154 mL	2.0385 mL
	60 mM	0.0679 mL	0.3397 mL	0.6795 mL	1.6987 mL
	80 mM	0.0510 mL	0.2548 mL	0.5096 mL	1.2741 mL
	100 mM	0.0408 mL	0.2038 mL	0.4077 mL	1.0192 mL

OR-1896

2 Cited Publications

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OR-1896

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Cell Death Library

Ion Channel Compound Library

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Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

3D Diverse Fragment Library

Apoptosis Compound Library

Membrane Transporter/Ion Channel Compound Library

Metabolism/Protease Compound Library

MedChemExpress（MCE）の使用を引用している文献 OR-1896

Phosphodiesterase (PDE) アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (2)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

OR-1896

Anti-Cardiovascular Disease Compound Library

Anti-Alzheimer's Disease Compound Library

Neuroprotective Compound Library

Neurodegenerative Disease-related Compound Library

Drug Metabolite Library

Anti-Colorectal Cancer Compound Library

Potassium Channel Compound Library

Human Metabolite Library

Antihypertensive Compound Library

Metabolic Enzyme Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Ion Channel Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

3D Diverse Fragment Library

Apoptosis Compound Library

Membrane Transporter/Ion Channel Compound Library

Metabolism/Protease Compound Library

MedChemExpress（MCE）の使用を引用している文献 OR-1896

Phosphodiesterase (PDE) アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (2)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

OR-1896 関連分類

HY-135746 関連分類