| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
Ebaresdax targets peroxynitrite (ONOO-), a potent reactive nitrogen species formed from the reaction of superoxide and nitric oxide. It acts as a peroxynitrite scavenger, inhibiting both SIN-1-induced peroxynitrite oxidation and peroxynitrite-mediated cytotoxicity. By neutralizing this deleterious oxidant, Ebaresdax reduces oxidative stress and inflammation without binding to opioid receptors, distinguishing it from traditional opioid analgesics.
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| ln Vitro |
In vitro, Ebaresdax inhibits SIN-1-induced peroxynitrite oxidation with an IC50 of 3.7 +/- 0.80 uM and peroxynitrite-mediated cytotoxicity with an IC50 of 0.13 +/- 0.02 uM. These activities demonstrate potent peroxynitrite scavenging capacity at sub-micromolar concentrations for cytoprotection. The compound shows good solubility in DMSO (50 mg/mL, 187.74 mM) and is stable as a powder at -20degC for up to 3 years.
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| ln Vivo |
In vivo, Ebaresdax has been evaluated in preclinical models of pain and inflammation, demonstrating efficacy as a non-opioid analgesic. It is orally bioavailable and has been investigated in Phase 2 clinical trials (NCT04855240) for acute postoperative pain following bunionectomy and (NCT05008835) for pain associated with osteoarthritis of the knee. The compound exhibits anti-inflammatory properties attributed to its peroxynitrite scavenging mechanism.
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| Enzyme Assay |
For in vitro assays, Ebaresdax is dissolved in DMSO to prepare a 10 mM stock solution (50 mg/mL, 187.74 mM). For peroxynitrite oxidation inhibition studies, the compound is incubated with SIN-1 (a peroxynitrite generator) in an appropriate buffer, and the oxidation product is measured spectrophotometrically at a specific wavelength (e.g., dihydrorhodamine 123 oxidation). The IC50 is calculated by nonlinear regression analysis of dose-response curves (concentrations typically 0.01-100 uM).
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| Cell Assay |
For in vitro cell-based cytotoxicity assays, cells (e.g., neuronal, endothelial, or immune cells) are cultured in standard medium (DMEM with 10% FBS, 1% penicillin-streptomycin) at 37degC with 5% CO2. Cells are seeded in 96-well plates at 5,000-10,000 cells/well and allowed to attach overnight. Peroxynitrite-mediated cytotoxicity is induced by SIN-1 (100-500 uM) in the presence or absence of Ebaresdax at varying concentrations (0.01-100 uM). After 24-48 hours of incubation, cell viability is assessed using MTT or Alamar Blue assays. IC50 values are calculated by dose-response curves.
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| Animal Protocol |
For in vivo preclinical studies, Ebaresdax is typically administered to rodents via oral gavage (since it is orally bioavailable) at doses ranging from 1-100 mg/kg depending on the model. For pain models (e.g., formalin test, CFA-induced inflammatory pain, or post-surgical pain), animals receive a single oral dose 30-60 minutes before pain assessment. Blood samples may be collected for PK analysis. For efficacy studies, behavioral pain responses (e.g., paw withdrawal threshold, latency) are measured using von Frey filaments or a plantar test apparatus.
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| Toxicity/Toxicokinetics |
Toxicology studies have not been published in detail for Ebaresdax, but as a clinical-stage drug candidate it has undergone preclinical safety evaluation. In vitro, it exhibits low cytotoxicity at concentrations below its therapeutic IC50, with a selectivity window demonstrated by the sub-micromolar IC50 for peroxynitrite-mediated cytotoxicity (0.13 uM). The compound has undergone Phase 2 clinical trials (NCT04855240, NCT05008835), indicating acceptable tolerability in human subjects. Standard safety precautions for handling investigational drugs apply.
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| References | |
| Additional Infomation |
Ebaresdax is a small molecule drug. The clinical trial NCT05008835 is currently underway (evaluating the efficacy and safety of ACP-044 in patients with knee osteoarthritis-related pain). The monoisotope molecular weight of Ebaresdax is 266.07 Da.
Ebaresdax is currently under clinical investigation and has not received regulatory approval for any indication. It has been studied in Phase 2 clinical trials: NCT04855240 (Evaluate the Efficacy and Safety of ACP-044 for the Treatment of Acute Postoperative Pain Following Bunionectomy) and NCT05008835 (Evaluate the Efficacy and Safety of ACP-044 in Subjects with Pain Associated with Osteoarthritis of the Knee). The maximum clinical trial phase completed is Phase II (across all indications). Ebaresdax is a first-in-class, non-opioid analgesic that functions as a peroxynitrite scavenger. |
| Molecular Formula |
C12H14N2O3S
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|---|---|
| Molecular Weight |
266.3162
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| Exact Mass |
266.072
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| CAS # |
1334471-39-4
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| Related CAS # |
Ebaresdax hydrochloride;1334385-87-3
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| PubChem CID |
53362112
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| Appearance |
White to off-white solid powder
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| LogP |
1.8
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
18
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| Complexity |
370
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| Defined Atom Stereocenter Count |
1
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| SMILES |
S1C(N([H])C2=C([H])C([H])=C([H])C([H])=C2O[H])=N[C@]([H])(C(=O)O[H])C1(C([H])([H])[H])C([H])([H])[H]
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| InChi Key |
OASISJWJIHWVKX-SECBINFHSA-N
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| InChi Code |
InChI=1S/C12H14N2O3S/c1-12(2)9(10(16)17)14-11(18-12)13-7-5-3-4-6-8(7)15/h3-6,9,15H,1-2H3,(H,13,14)(H,16,17)/t9-/m1/s1
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| Chemical Name |
(4R)-2-(2-hydroxyanilino)-5,5-dimethyl-4H-1,3-thiazole-4-carboxylic 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: 50 mg/mL (187.74 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.39 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 (9.39 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 (9.39 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 | 3.7549 mL | 18.7744 mL | 37.5488 mL | |
| 5 mM | 0.7510 mL | 3.7549 mL | 7.5098 mL | |
| 10 mM | 0.3755 mL | 1.8774 mL | 3.7549 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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