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1mg |
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5mg |
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10mg |
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Other Sizes |
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Patamostat (E-3123) is a novel and potent protease inhibitor with the potential to be used for acute pancreatitis and disseminated intravascular coagulation. It has in vivo and in vitro inhibitory activity against trypsin, thrombin, plasmin, cathepsin-B and kallikrein with IC50s of 39 nM, 950 nM and 1.9 μM, respectively.
ln Vivo |
Pamostat (intravenous infusion) decreases mortality following induced pancreatitis in a dose-dependent manner, whether administered to rats at 0.03-0.3 mg/kg or to rabbits at 0.3-3.0 mg/kg in [1]. Dogs with pancreatitis see a decrease in serum trypsin and lipase activity when their intravenous infusion of Pamestat (1.0–3.0 mg/kg) is administered [1]. When administered continuously, patamostat (2 mg/kg/h) improves almost all measures in male Wistar rats, including plasma endotoxin and serum FDP levels, as well as mortality, serum and ascitic fluid amylase levels, and lysosomal enzyme profiles [2].
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Animal Protocol |
Animal/Disease Models: Male Wistar rats, weighing approximately 350 g [2]
Doses: 2 mg/kg Route of Administration: Continuous infusion every hour for 1 hour Experimental Results: Dramatically improved survival rate. |
References |
[1]. K Miyamoto, et al. [Effects of E-3123, a New Protease Inhibitor, on Several Protease Activities and on Experimental Acute Pancreatitis]. Nihon Yakurigaku Zasshi. 1988 May;91(5):285-93.
[2]. T Hirano, et al. Protective Effect of a Cephalosporin, Shiomarin, Plus a New Potent Protease Inhibitor, E3123, on Rat Taurocholate-Induced Pancreatitis. J Gastroenterol Hepatol. Jan-Feb 1993;8(1):52-9. |
Molecular Formula |
C₂₀H₂₀N₄O₄S
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Molecular Weight |
412.46
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CAS # |
114568-26-2
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Related CAS # |
Patamostat mesylate;114568-32-0
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O=C(OC1=CC=C(SCCN2C(CCC2=O)=O)C=C1)C3=CC=C(NC(N)=N)C=C3
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InChi Key |
ILRQPCQIFIURTG-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C20H20N4O4S/c21-20(22)23-14-3-1-13(2-4-14)19(27)28-15-5-7-16(8-6-15)29-12-11-24-17(25)9-10-18(24)26/h1-8H,9-12H2,(H4,21,22,23)
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Chemical Name |
Benzoic acid, 4-((aminoiminomethyl)amino)-, 4-((2-(2,5-dioxo-1-pyrrolidinyl)ethyl)thio)phenyl ester
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Synonyms |
PatamostatE-3123 E 3123 E3123
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ~100 mg/mL (~242.45 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.06 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.06 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.06 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.4245 mL | 12.1224 mL | 24.2448 mL | |
5 mM | 0.4849 mL | 2.4245 mL | 4.8490 mL | |
10 mM | 0.2424 mL | 1.2122 mL | 2.4245 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.