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Art. -Nr.: HY-182406

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CU-2010

CU-2010 is a synthetic low-molecular-weight serine protease inhibitor with anticoagulant, antifibrinolytic, anti-inflammatory, and cardioprotective properties. CU-2010 inhibits plasma kallikrein, factor Xa, and factor XIa activity. CU-2010 reduces free radical generation, lipid peroxidation, and postoperative blood loss; improves postischemic myocardial contractility, coronary blood flow, and endothelium-dependent vasodilatation; prolongs clotting and clot lysis times; and preserves clot firmness. CU-2010 can be used for the research of postoperative blood loss and postischemic myocardial dysfunction after cardiac surgery with cardiopulmonary bypass.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 1021707-76-5
Formel: C₃₇H₄₂N₆O₆S
Molecular Weight:698.83

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

CU-2010 Chemical Structure

CAS. Nr.: 1021707-76-5

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Use of MCE Products

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

HTRA1

In Vitro

CU-2010 (100-1000 nM) prolongs intrinsic and extrinsic clotting times in a concentration-dependent manner and preserves clot strength in citrated human whole blood at concentrations of 100 to 1000 nM^[1].

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

In Vivo

CU-2010 (0.5-1.66 mg/kg; i.v.; slow infusion over 90 minutes) dose-dependently reduces postoperative blood loss by up to 91% (1.66 mg/kg dose) compared to control, preserves coronary blood flow and myocardial contractility (with 1.66 mg/kg restoring ESPVR to 118% of baseline), and reduces oxidative stress, with greater cardioprotective effects than aprotinin at higher doses^[1].

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

Animal Model:

Foxhound (weighing 22 to 35 kg)^[1]
Dosage:

0.5 mg/kg; 0.83 mg/kg; 1.25 mg/kg; 1.66 mg/kg
Administration:

i.v.; slow infusion over 90 minutes
Result:

Reduced postoperative blood loss (first 2 hours after protamine) dose-dependently to 95 mL (0.5 mg/kg), 57 mL (0.83 mg/kg), 46 mL (1.25 mg/kg), 13 mL (1.66 mg/kg), all P<.05 vs control.
Slightly elevated activated clotting time (ACT) and remarkably elevated activated partial thromboplastin time (aPTT) in all CU-2010 groups compared to control and aprotinin groups.
Prolonged extrinsic system (EXTEM) clotting time (CT) to 58 s (0.5 mg/kg), 86 s (0.83 mg/kg), 82 s (1.25 mg/kg), 51 s (1.66 mg/kg), all P<.05 vs control and aprotinin.
Extended extrinsic system (EXTEM) lysis time (LT) to >3600 s (0.5, 0.83, 1.25 mg/kg) and 3290 s (1.66 mg/kg), with no clot lysis observed within the measurement period for all CU-2010 doses.
Prolonged intrinsic system (INTEM) clotting time (CT) to 845 s (0.5 mg/kg), 1587 s (0.83 mg/kg), 1520 s (1.25 mg/kg), 823 s (1.66 mg/kg), all P<.05 vs control and aprotinin.
Reduced intrinsic system (INTEM) maximum clot strength (MCF) to 41 mm (0.5 mg/kg), 45 mm (0.83 mg/kg), 30 mm (1.25 mg/kg), 47 mm (1.66 mg/kg), all P<.05 vs baseline, with 1.25 mg/kg also P<.05 vs aprotinin.
Preserved coronary blood flow (CBF) at 51 mL/min (0.5 mg/kg), 42 mL/min (0.83 mg/kg), 47 mL/min (1.25 mg/kg), 37 mL/min (1.66 mg/kg), all P<.05 vs control.
Preserved slope of the end-systolic pressure-volume relationship (ESPVR) at 2.32 mm Hg/mL (0.5 mg/kg), 2.81 mm Hg/mL (0.83 mg/kg), 3.57 mm Hg/mL (1.25 mg/kg), 2.96 mm Hg/mL (1.66 mg/kg), with 1.66 mg/kg P<.05 vs control.
Achieved 118% percent recovery of ESPVR at 1.66 mg/kg, P<.05 vs control.
Preserved preload recruitable stroke work (PRSW) at 48 kerg (0.5 mg/kg), 40 kerg (0.83 mg/kg), 55 kerg (1.25 mg/kg), 57 kerg (1.66 mg/kg), with 1.25 and 1.66 mg/kg P<.05 vs aprotinin.
Achieved 108% percent recovery of PRSW at 1.25 mg/kg and 105% at 1.66 mg/kg, both P<.05 vs control and aprotinin.
Preserved coronary endothelial function (vasodilative response to acetylcholine) to levels comparable to aprotinin across all CU-2010 doses, preventing the reduction seen in controls.
Reduced cardiac tissue malonaldehyde (MDA) levels to 2.9 μmol/L/g dry weight (0.5 mg/kg), 3.1 μmol/L/g dry weight (0.83 mg/kg), 2.4 μmol/L/g dry weight (1.25 mg/kg), 1.9 μmol/L/g dry weight (1.66 mg/kg), all P<.05 vs control; 1.66 mg/kg also P<.05 vs aprotinin.

Related Protocols :

Chemical Information

CAS. Nr. 1021707-76-5
Molecular Weight 698.83
Formel C₃₇H₄₂N₆O₆S
SMILES

NCC1=CC=CC(C[C@@H](C(NCC2=CC=C(C=C2)C(N)=N)=O)NC([C@@H](CCCC3=CC=CC=C3)NS(CC4=CC(C(O)=O)=CC=C4)(=O)=O)=O)=C1
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Szabó G, et al. The novel synthetic serine protease inhibitor CU-2010 dose-dependently reduces postoperative blood loss and improves postischemic recovery after cardiac surgery in a canine model. J Thorac Cardiovasc Surg. 2010;139(3):732-740. [Content Brief]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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.

Bioz

MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

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CU-2010