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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1021707-76-5
- 分子式: C37H42N6O6S
- 分子量:698.83
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
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Serine protease |
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.
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: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.
化学情報
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CAS 番号 1021707-76-5
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分子量 698.83
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)