| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 500mg |
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| Targets |
1,4-DPCA ethyl ester targets factor inhibiting HIF (FIH), an enzyme that hydroxylates HIF-1α and inhibits its transcriptional activity. By inhibiting FIH, 1,4-DPCA ethyl ester stabilizes HIF-1α and promotes HIF-1 transcriptional activity. It is a prodrug form of 1,4-DPCA, a prolyl 4-hydroxylase inhibitor. 1,4-DPCA ethyl ester also has activity against M. tuberculosis.
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|---|---|
| ln Vitro |
1,4-DPCA ethyl ester is a tricyclic substance that suppresses the regulatory factor HIF (FIH) [1].
In vitro, 1,4-DPCA ethyl ester inhibits FIH. It has potential anticancer activity based on growth inhibition assays. It is active against M. tuberculosis with an MIC90 of 23.99 µM. 1,4-DPCA ethyl ester is a synthetic precursor of the prolyl 4-hydroxylase inhibitor 1,4-DPCA. |
| ln Vivo |
In vivo, 1,4-DPCA ethyl ester has shown promise in regenerative medicine and ischemic disease models by enhancing vascularization, reducing inflammation, and promoting tissue repair through controlled HIF-1α activation under normoxic conditions. However, specific published in vivo efficacy studies are not detailed in the current literature.
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| Enzyme Assay |
The in vitro FIH inhibition assay for 1,4-DPCA ethyl ester uses recombinant FIH enzyme and a HIF-1α peptide substrate. Enzyme activity is measured by quantifying the hydroxylation of the substrate using mass spectrometry or antibody-based methods. IC50 values are calculated from dose-response curves. Antimycobacterial activity is assessed using broth microdilution methods.
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| Cell Assay |
Cellular assays for 1,4-DPCA ethyl ester are conducted in various cell lines. Cells are treated with varying concentrations of 1,4-DPCA ethyl ester. HIF-1α protein levels are measured by Western blotting. HIF-1 transcriptional activity is assessed using reporter gene assays. Cell proliferation and viability are measured using standard assays such as MTT or CellTiter-Glo.
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| Animal Protocol |
In vivo studies for 1,4-DPCA ethyl ester would typically involve animal models of ischaemic disease or cancer. The compound would be administered via intraperitoneal or oral routes. Efficacy would be assessed by measuring vascularization, inflammation, tissue repair, or tumor growth. However, specific published in vivo protocols for 1,4-DPCA ethyl ester are not available in the current literature.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for 1,4-DPCA ethyl ester is not extensively reported. The compound has a molecular weight of 268.27 g/mol and a molecular formula of C15H12N2O3. It is soluble in DMF, DMSO, and ethanol. As a small molecule, it is expected to have moderate bioavailability. Detailed PK parameters such as half-life and bioavailability are not available.
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| Toxicity/Toxicokinetics |
Toxicity data for 1,4-DPCA ethyl ester is limited. As a research compound, 1,4-DPCA ethyl ester is intended for research use only and not for human therapeutic applications. Standard in vitro cytotoxicity assays and in vivo tolerability studies would be required for a complete toxicity assessment.
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| References | |
| Additional Infomation |
1,4-DPCA ethyl ester (CAS 86443-19-8) is a synthetic precursor of the prolyl 4-hydroxylase inhibitor 1,4-DPCA. It inhibits FIH and has potential anticancer activity. It has a molecular formula of C15H12N2O3 and a molecular weight of 268.27 g/mol. 1,4-DPCA ethyl ester is for research use only.
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| Molecular Formula |
C15H12N2O3
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|---|---|
| Molecular Weight |
268.267
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| Exact Mass |
268.085
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| CAS # |
86443-19-8
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| PubChem CID |
327508
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
2.253
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
20
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| Complexity |
446
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
YUPWGIFULUYTQG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H12N2O3/c1-2-20-15(19)11-8-17-13-10(14(11)18)6-5-9-4-3-7-16-12(9)13/h3-8H,2H2,1H3,(H,17,18)
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| Chemical Name |
ethyl 4-oxo-1H-1,10-phenanthroline-3-carboxylate
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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 : ~20.83 mg/mL (~77.65 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.75 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 20.8 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: ≥ 2.08 mg/mL (7.75 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7276 mL | 18.6379 mL | 37.2759 mL | |
| 5 mM | 0.7455 mL | 3.7276 mL | 7.4552 mL | |
| 10 mM | 0.3728 mL | 1.8638 mL | 3.7276 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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