| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg | |||
| 100mg | |||
| 250mg | |||
| 500mg | |||
| Other Sizes |
| Targets |
5-Lipoxygenase (5-LO), 12-LO, 15-LO
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|---|---|
| ln Vitro |
Transendothelial dextran transport was markedly enhanced by either high glucose or 12(S)-HETE, and it was further enhanced by the combination of the two. Glucan transport was only partially inhibited by the addition of the 12/15-LO inhibitor CDC [1].
CDC is a potent and direct inhibitor of 5-LO (5-Lipoxygenase) that reduces 5-LO activity in cell-free assays. CDC also inhibits 12-LO and 15-LO. As a 12/15-LO inhibitor, CDC can counteract the effects of elevated glucose on protein phosphorylation, thereby reducing the disruption of the endothelium cell barrier in mice. Lipoxygenases are key enzymes in the biosynthesis of leukotrienes and other lipid mediators of inflammation, making them important targets for anti-inflammatory drug development. |
| ln Vivo |
Elevated glucose and 12(S)-hydroxyeicosatetraenoic acid (HETE) can modify the phosphorylation levels of β-catenin and vascular endothelial (VE)-cadherin, but not the expression of all proteins. Cinnamyl-3,4-dihydroxy-α-cyanocinnamate (CDC), a 12/15-LO inhibitor, can counteract the effects of elevated glucose on protein phosphorylation, therefore reducing the disruption of the endothelium cell barrier in mice. Diabetes models added to the validation of these findings [1].
CDC can counteract the effects of elevated glucose on protein phosphorylation, thereby reducing the disruption of the endothelium cell barrier in mice. This activity suggests potential therapeutic applications in diabetic complications and vascular disease. By inhibiting lipoxygenases, CDC may reduce inflammation, oxidative stress, and vascular dysfunction. |
| Enzyme Assay |
Lipoxygenase enzyme activity is measured using cell-free assays with recombinant 5-LO, 12-LO, or 15-LO enzymes and appropriate substrates. Inhibition of enzyme activity is determined by measuring the production of lipoxygenase products. IC50 values are determined from dose-response curves.
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| Cell Assay |
Cellular potency is evaluated in endothelial cells or other relevant cell types by measuring lipoxygenase activity and its effects on protein phosphorylation. Cells are treated with CDC at various concentrations, and lipoxygenase product formation is measured. Effects on glucose-induced protein phosphorylation and endothelial barrier function are assessed.
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| Animal Protocol |
In vivo efficacy is evaluated in mouse models of endothelial dysfunction or diabetic complications. CDC is administered via appropriate routes at various doses. Endothelial barrier function is assessed, and markers of inflammation and oxidative stress are measured. The compound's ability to counteract the effects of elevated glucose on the endothelium is evaluated.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for CDC are limited as the compound is primarily used as a research tool. The compound is soluble in appropriate solvents for formulation. Detailed PK parameters such as half-life, clearance, and bioavailability are available from preclinical studies.
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| Toxicity/Toxicokinetics |
Comprehensive toxicological data for CDC are limited as the compound is primarily used for research purposes. Standard laboratory safety precautions should be observed during handling. The compound is not intended for human therapeutic use and has not been evaluated in formal toxicology studies.
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| References | |
| Additional Infomation |
CDC (Cinnamyl-3,4-dihydroxy-α-cyanocinnamate) is a research tool for studying lipoxygenase function in inflammation, vascular biology, and diabetic complications. The compound inhibits 5-LO, 12-LO, and 15-LO, making it a broad-spectrum lipoxygenase inhibitor. CDC can counteract the effects of elevated glucose on protein phosphorylation and reduce endothelial barrier disruption. The compound's molecular formula is C19H15NO4 with a molecular weight of 321.33.
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| Molecular Formula |
C19H15NO4
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|---|---|
| Molecular Weight |
321.332
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| Exact Mass |
321.1
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| Elemental Analysis |
C, 71.02; H, 4.71; N, 4.36; O, 19.92
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| CAS # |
132465-11-3
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| PubChem CID |
14840979
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| Appearance |
White to yellow solid powder
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| Density |
1.326 g/cm3
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| Boiling Point |
583.9ºC at 760 mmHg
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| Flash Point |
307ºC
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| LogP |
3.261
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
24
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| Complexity |
525
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C(/C=C/COC(/C(/C#N)=C/C2=CC(O)=C(O)C=C2)=O)C=C1
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| InChi Key |
XGHYFEJMJXGPGN-UYHGDYIZSA-N
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| InChi Code |
InChI=1S/C19H15NO4/c20-13-16(11-15-8-9-17(21)18(22)12-15)19(23)24-10-4-7-14-5-2-1-3-6-14/h1-9,11-12,21-22H,10H2/b7-4+,16-11+
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| Chemical Name |
3-Phenyl-2-propen-1-yl (2E)-2-cyano-3-(3,4-dihydroxyphenyl)-2-propenoate
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| Synonyms |
Cinnamyl-3,4-dihydroxy-α-cyanocinnamate; CDC 5-LO inhibitor; CDC lipoxygenase inhibitor
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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 : ~50 mg/mL (~155.60 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.78 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 (7.78 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1121 mL | 15.5603 mL | 31.1207 mL | |
| 5 mM | 0.6224 mL | 3.1121 mL | 6.2241 mL | |
| 10 mM | 0.3112 mL | 1.5560 mL | 3.1121 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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