2. Metabolic Enzyme/Protease
  3. Ser/Thr Protease
  4. CU-2010

CU-2010 is a Serine protease inhibitor. In canine models, CU-2010 reduces blood loss after cardiac surgery in a dose-dependent manner and improves post-ischemic recovery.

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CU-2010

CU-2010 Chemical Structure

CAS No. : 1021707-76-5

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CU-2010 Related Antibodies

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Description

CU-2010 is a Serine protease inhibitor. In canine models, CU-2010 reduces blood loss after cardiac surgery in a dose-dependent manner and improves post-ischemic recovery[1].

IC50 & Target[1]

Serine protease

 

In Vitro

CU-2010 (100-1000 nM) progressively delays blood coagulation induced by both tissue factor and contact phase stimulation[1].

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

CU-2010 Related Antibodies
In Vivo

CU-2010 (0.5-1.66 mg/kg; slow infusion over 90 min) reduces postoperative blood loss in a dose-dependent manner; it also maintains coronary blood flow and myocardial contractile function, and alleviates oxidative stress[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: 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.
Molecular Weight

698.83

Formula

C37H42N6O6S
CAS No.
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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Room temperature in continental US; may vary elsewhere.
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Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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CU-2010 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CU-20101021707-76-5CU2010CU 2010Ser/Thr ProteaseSerine proteasesSerine endopeptidasesThreonine proteasespostoperative blood losscardiopulmonary bypassfactor Xaplasma kallikreincardiac surgerypostischemic myocardial dysfunctionfactor XIaoxidative stressendothelium-dependent vasodilatationhuman whole bloodInhibitorinhibitorinhibit

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