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.
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- CAS No.: 1021707-76-5
- 화학식: C37H42N6O6S
- 분자량:698.83
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
[1]|
HTRA1 |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Foxhound (weighing 22 to 35 kg)[1]
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Dosage:0.5 mg/kg; 0.83 mg/kg; 1.25 mg/kg; 1.66 mg/kg
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Administration:i.v.; slow infusion over 90 minutes
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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.
Chemical Information
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CAS No. 1021707-76-5
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분자량 698.83
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화학식 C37H42N6O6S
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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
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CU-2010 Related Classifications
HY-182406 Related Classifications
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Keywords
- CU-2010
- 1021707-76-5
- CU2010
- CU 2010
- Ser/Thr Protease
- Serine proteases
- Serine endopeptidases
- Threonine proteases
- postoperative blood loss
- factor Xa
- postischemic myocardial contractility
- plasma kallikrein
- lipid peroxidation
- postischemic myocardial dysfunction
- free radical generation
- coronary blood flow
- factor XIa
- endothelium-dependent vasodilatation
- Inhibitor
- inhibitor
- inhibit