| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
| Targets |
Soluble epoxide hydrolase (sEH) - potent, orally active inhibitor (IC50 = 0.04 nM).
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| ln Vitro |
In vitro enzymatic assays demonstrate that EC-5026 is a potent inhibitor of soluble epoxide hydrolase (sEH) with an IC50 of 0.04 nM. sEH is an enzyme that metabolizes epoxyeicosatrienoic acids (EETs), which are lipid signaling molecules with anti-inflammatory and analgesic properties. By inhibiting sEH, EC-5026 increases the levels of EETs, which promote the resolution of inflammation and exert pain-relieving effects. The compound's potent inhibition of sEH and its oral bioavailability make it a promising candidate for pain management.
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| ln Vivo |
EC5026 (BPN-19186) soothes pain in dogs, cats, and horses that occurs naturally and has demonstrated effectiveness in treating pain in experimental animals without showing any negative or addictive consequences [1].
In vivo studies have demonstrated that EC-5026 soothes pain in dogs, cats, and horses that occurs naturally and has demonstrated effectiveness in treating pain in experimental animals without showing any negative or addictive consequences. The compound shows efficacy for inflammatory and neuropathic pain. By inhibiting sEH and increasing EET levels, EC-5026 promotes the resolution of inflammation and exerts analgesic effects without the risks associated with opioid-based therapies. These findings support the potential of EC-5026 as a novel, non-opioid analgesic for the treatment of chronic pain conditions. |
| Enzyme Assay |
sEH enzymatic activity assays are performed using purified recombinant sEH enzyme and a suitable substrate such as 14,15-EET or a fluorogenic substrate. The enzyme is incubated with the substrate and varying concentrations of EC-5026, and the formation of the diol product is measured by HPLC or fluorescence. IC50 values are calculated from dose-response curves. Selectivity against other epoxide hydrolases and related enzymes is assessed using similar biochemical assay formats to confirm the compound's specificity for sEH.
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| Cell Assay |
Cellular assays for EC-5026 typically involve culturing cells relevant to inflammation and pain, such as macrophages, neurons, or glial cells. Cells are treated with the compound at various concentrations, and sEH activity is assessed by measuring EET metabolism or by measuring the levels of EETs and their diol metabolites. Inflammatory responses are assessed by measuring cytokine production (TNF-α, IL-1β, IL-6) by ELISA. Neuronal excitability is assessed using patch-clamp electrophysiology or calcium imaging. Cytotoxicity against mammalian cells is assessed in parallel to evaluate selectivity.
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| Animal Protocol |
In vivo efficacy of EC-5026 is evaluated in animal models of inflammatory and neuropathic pain. For inflammatory pain, models such as carrageenan-induced paw edema or complete Freund's adjuvant (CFA)-induced inflammation are used. For neuropathic pain, models such as spinal nerve ligation or chemotherapy-induced neuropathy are used. Animals are treated with EC-5026 via oral administration, and pain behavior is assessed using mechanical allodynia (von Frey test), thermal hyperalgesia (Hargreaves test), or other pain-related behavioral tests. Inflammation is assessed by measuring paw edema or cytokine levels. The compound's analgesic and anti-inflammatory effects are quantified. Pharmacokinetic studies are conducted to determine the compound's bioavailability and tissue distribution.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of EC-5026 have been characterized to support its use as an orally active research tool and potential therapeutic agent. The compound has a molecular weight of 405.39 and the molecular formula C18H23F4N3O3. Key PK parameters including half-life, clearance, volume of distribution, and oral bioavailability are determined using LC-MS/MS analysis of plasma and tissue samples following oral administration. The compound's ability to reach the central nervous system and peripheral sites of inflammation is important for its analgesic and anti-inflammatory efficacy. The compound's favorable pharmacokinetic profile supports its potential for further development as a non-opioid analgesic.
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| Toxicity/Toxicokinetics |
Toxicological evaluation of EC-5026 is typically conducted in parallel with efficacy studies in animal models. Standard toxicology assessments include in vitro cytotoxicity assays against a panel of mammalian cell lines to determine the compound's selectivity index. In vivo toxicity studies in rodents include acute and repeated-dose toxicity testing, observation of clinical signs and body weight changes, and histopathological examination of major organs. As an sEH inhibitor that modulates lipid signaling, potential effects on blood pressure, inflammation, and pain processing are carefully monitored. The compound's non-opioid mechanism of action suggests a favorable safety profile with reduced risk of addiction and dependence.
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| References | |
| Additional Infomation |
EC-5026 is a research tool compound and potential therapeutic agent used for studying the role of soluble epoxide hydrolase in pain and inflammation. The compound is not approved for clinical use and is intended for laboratory research purposes only. Its mechanism of action involves potent inhibition of sEH, which increases the levels of anti-inflammatory and analgesic EETs and promotes the resolution of inflammation. EC-5026 is a first-in-class, non-opioid, and orally active sEH inhibitor that shows efficacy for inflammatory and neuropathic pain. This compound is valuable for validating sEH as a therapeutic target for pain management and for developing non-opioid analgesics.
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| Molecular Formula |
C18H23F4N3O3
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|---|---|
| Molecular Weight |
405.387138605118
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| Exact Mass |
405.167
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| CAS # |
1809885-32-2
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| Related CAS # |
(Rac)-EC5026;1809885-55-9
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| PubChem CID |
91933845
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| Appearance |
White to off-white solid powder
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| LogP |
3.7
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
28
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| Complexity |
539
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| Defined Atom Stereocenter Count |
1
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| SMILES |
FC1=C(C=CC(=C1)NC(NC1CCN(C([C@@H](C)CC)=O)CC1)=O)OC(F)(F)F
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| InChi Key |
LHRXHTKENPCGSZ-NSHDSACASA-N
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| InChi Code |
InChI=1S/C18H23F4N3O3/c1-3-11(2)16(26)25-8-6-12(7-9-25)23-17(27)24-13-4-5-15(14(19)10-13)28-18(20,21)22/h4-5,10-12H,3,6-9H2,1-2H3,(H2,23,24,27)/t11-/m0/s1
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| Chemical Name |
(S)-1-(3-fluoro-4-(trifluoromethoxy)phenyl)-3-(1-(2-methylbutanoyl)piperidin-4-yl)urea
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| Synonyms |
BPN-19186 EC5026BPN 19186 EC 5026BPN19186 EC-5026
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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 : ≥ 250 mg/mL (~616.69 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.13 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 (5.13 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 20.8 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: ≥ 2.08 mg/mL (5.13 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 | 2.4668 mL | 12.3338 mL | 24.6676 mL | |
| 5 mM | 0.4934 mL | 2.4668 mL | 4.9335 mL | |
| 10 mM | 0.2467 mL | 1.2334 mL | 2.4668 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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