| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Targets |
EP1013 targets caspases, a family of cysteine-aspartic proteases that play essential roles in apoptosis and inflammation. As a broad-spectrum caspase inhibitor, it blocks the activity of multiple caspase family members. By inhibiting caspase activity, EP1013 may help regulate cell death processes and potentially offer therapeutic benefits in the context of type 1 diabetes.
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| ln Vitro |
In vitro, EP1013 is a broad-spectrum selective inhibitor of caspases. Its inhibitory activity is typically assessed in caspase activity assays using fluorogenic or chromogenic substrates. The compound's potency and selectivity profile against different caspase family members can be determined. EP1013 is used as a research tool to study the role of caspases in apoptosis and inflammation.
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| ln Vivo |
The marginal islet mass function was dramatically improved by EP1013 (1, 3, 10 mg/kg). Primary islet graft nonfunction was observed in two animals in the 10 mg/kg EP1013-treated group; nevertheless, the diabetes reversal rate in this group was not comparable to that of the 3 mg/kg EP1013, 1 mg/kg EP1013, or 10 mg/kg zVAD groups. notable variations. EP1013 therapy prolongs islet graft function and increases functional syngeneic islet mass [1].
In vivo, EP1013 therapy enhances functional syngeneic islet mass and promotes longevity of islet graft function. EP1013 (1, 3, 10 mg/kg) significantly improves marginal islet mass function. Two animals in the 10 mg/kg EP1013 treatment group exhibit primary islet graft nonfunction, but the diabetes reversal rate for this group is not significantly different from the 3 mg/kg EP1013, 1 mg/kg EP1013, or 10 mg/kg zVAD groups. These results support its potential for type 1 diabetes research. |
| Enzyme Assay |
For in vitro enzyme assays, EP1013 is evaluated using caspase activity assays. The compound is incubated with recombinant caspases and fluorogenic or chromogenic substrates at various concentrations. Caspase activity is quantified by measuring the release of fluorophore or chromophore. IC₅0 values are determined from dose-response curves. Selectivity profiling against different caspase family members can be performed to characterize the compound's broad-spectrum activity.
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| Cell Assay |
For in vitro cellular experiments, EP1013 is tested in cell lines to evaluate its effects on apoptosis and inflammation. Cells are cultured in appropriate media and treated with various concentrations of the compound. Caspase activity is assessed by measuring cleavage of caspase substrates using Western blotting or fluorescence-based assays. Apoptosis is evaluated using Annexin V staining or other apoptosis markers. The compound's effects on cell viability are monitored.
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| Animal Protocol |
For in vivo animal experiments, EP1013 can be administered to rodents via various routes including intraperitoneal injection or oral gavage. The compound's efficacy can be evaluated in models of type 1 diabetes or islet transplantation. EP1013 (1, 3, 10 mg/kg) significantly improves marginal islet mass function. Islet graft function and diabetes reversal are assessed.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of EP1013 are not extensively detailed in the public literature. As a small molecule with a molecular weight of 382.38, it may have reasonable bioavailability and tissue distribution. The compound is soluble in DMSO at 60 mg/mL. Detailed parameters such as Cₘₐₓ, Tₘₐₓ, AUC, half-life, and clearance would need to be determined through comprehensive PK studies.
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| Toxicity/Toxicokinetics |
Toxicological data for EP1013 are limited, as it is primarily a research tool. As a caspase inhibitor, its toxicity would depend on the importance of caspases for normal cellular function and immune homeostasis. Comprehensive toxicology studies including acute and repeated-dose toxicity, genotoxicity, and immunotoxicity assessments would be needed for further development. Appropriate safety precautions should be taken when handling this compound.
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| References | |
| Additional Infomation |
EP1013 is a research compound used to study caspase biology and develop therapies for type 1 diabetes. No clinical trials or regulatory approvals have been reported for this compound as a therapeutic agent. It is available from various chemical suppliers for research purposes only. The compound is a broad-spectrum caspase selective inhibitor that enhances islet graft function.
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| Molecular Formula |
C₁₈H₂₃FN₂O₆
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|---|---|
| Molecular Weight |
382.38
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| Exact Mass |
382.154
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| CAS # |
223568-55-6
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| PubChem CID |
9907987
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
639.8±55.0 °C at 760 mmHg
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| Flash Point |
340.7±31.5 °C
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| Vapour Pressure |
0.0±2.0 mmHg at 25°C
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| Index of Refraction |
1.523
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| LogP |
2.88
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
27
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| Complexity |
534
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CC(C)[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)CF)NC(=O)OCC1=CC=CC=C1
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| InChi Key |
LYBWGROBJJXCJJ-BBRMVZONSA-N
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| InChi Code |
InChI=1S/C18H23FN2O6/c1-11(2)16(17(25)20-13(8-15(23)24)14(22)9-19)21-18(26)27-10-12-6-4-3-5-7-12/h3-7,11,13,16H,8-10H2,1-2H3,(H,20,25)(H,21,26)(H,23,24)/t13-,16-/m0/s1
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| Chemical Name |
(3S)-5-fluoro-3-[[(2S)-3-methyl-2-(phenylmethoxycarbonylamino)butanoyl]amino]-4-oxopentanoic acid
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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 |
| 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 (~261.52 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.54 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 (6.54 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 (6.54 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 | 2.6152 mL | 13.0760 mL | 26.1520 mL | |
| 5 mM | 0.5230 mL | 2.6152 mL | 5.2304 mL | |
| 10 mM | 0.2615 mL | 1.3076 mL | 2.6152 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.
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