CU-2010 (100-1000 nM) gradually delays blood clotting caused by tissue factor and contact period stimulation[1].

CU-2010 (0.5-1.66 mg/kg; slow infusion over 90 minutes) reduces postoperative blood loss in a dose-dependent manner; it also maintains coronary blood flow and myocardial contractility and reduces oxidative stress [1].

Animal/Disease Models:Foxhound (weight 22 to 35 kg) [1]
Doses: 0.5 mg/kg; 0.83 mg/kg; 1.25 mg/kg; 1.66 mg/kg
Route of Administration: Intravenous injection; slow infusion over 90 minutes
Experimental Results: Compared with the control group and the aprotinin group, the activated clotting time (ACT) was slightly increased in all CU-2010 groups, and the activated partial thromboplastin time (aPTT) was significantly increased. The extrinsic coagulation system (EXTEM) clotting time (CT) was prolonged to 58 seconds (0.5 mg/kg), 86 seconds (0.83 mg/kg), 82 seconds (1.25 mg/kg) and 51 seconds (1.66 mg/kg), respectively. All P values were < 0.05 compared with the control group and the aprotinin group. The extrinsic hemolytic system (EXTEM) hemolysis time (LT) was prolonged to >3600 seconds (0.5, 0.83, 1.25 mg/kg) and 3290 seconds (1.66 mg/kg), respectively, with no thrombolysis observed in any of the CU-2010 dose groups during the measurement period. The intrinsic coagulation system (INTEM) clotting time (CT) was prolonged to 845 seconds (0.5 mg/kg), 1587 seconds (0.83 mg/kg), 1520 seconds (1.25 mg/kg), and 823 seconds (1.66 mg/kg), respectively, with all P < 0.05 compared to the control and aprotinin groups. The maximum clot strength (MCF) of the intrinsic coagulation system (INTEM) decreased to 41 mm (0.5 mg/kg), 45 mm (0.83 mg/kg), 30 mm (1.25 mg/kg), and 47 mm (1.66 mg/kg), all P < 0.05 compared to baseline, with the 1.25 mg/kg group also showing P < 0.05 compared to the aprotinin group. Coronary blood flow (CBF) remained stable at 51 mL/min (0.5 mg/kg), 42 mL/min (0.83 mg/kg), 47 mL/min (1.25 mg/kg), and 37 mL/min (1.66 mg/kg), P < 0.05 compared to the control group. The end-systolic pressure-volume relationship slope (ESPVR) remained stable at 2.32 mmHg/mL (0.5 mg/kg), 2.81 mmHg/mL (0.83 mg/kg), 3.57 mmHg/mL (1.25 mg/kg), and 2.96 mmHg/mL (1.66 mg/kg), with the 1.66 mg/kg group showing a significant difference compared to the control group (P<0.05). The ESPVR recovery rate in the 1.66 mg/kg group reached 118%, which was significantly higher than that in the control group (P<0.05). At doses of CU-2010 of 48 kerg (0.5 mg/kg), 40 kerg (0.83 mg/kg), 55 kerg (1.25 mg/kg), and 57 kerg (1.66 mg/kg), preload-recruitable stroke function (PRSW) was maintained, with significant differences compared to the aprotinin group (P<0.05) at the 1.25 mg/kg and 1.66 mg/kg groups. The PRSW recovery rate reached 108% in the 1.25 mg/kg group and 105% in the 1.66 mg/kg group, both significantly lower than the control and aprotinin groups (P<0.05). At all CU-2010 doses, coronary endothelial function (vasodilatory response to acetylcholine) was maintained at levels comparable to aprotinin, avoiding the endothelial function decline observed in the control group. Malondialdehyde (MDA) levels in cardiac tissue decreased 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), and 1.9 μmol/L/g dry weight (1.66 mg/kg), all P < 0.05 compared to the control group; 1.66 mg/kg also P < 0.05 compared to aprotinin.

[1]. 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.

C37H42N6O6S

698.83

1021707-76-5

Typically exists as solids at room temperature

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

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)