| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
P2X7 receptor (stated as a P2X7 receptor antagonist developed for the treatment of rheumatoid arthritis; no specific IC50, Ki, or EC50 values provided in this paper) [1]
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| ln Vitro |
EVT-401 acts as a purinergic P2X7 receptor antagonist. The compound exhibits good solubility in DMSO (100 mg/mL) and can be formulated for cell-based assays using appropriate dissolution methods. It has been shown to have efficacy in combating neuroinflammation in vitro. Detailed IC50 data for EVT-401 are not specified in the available literature; however, the compound's mechanism involves blocking the P2X7 receptor, thereby inhibiting downstream inflammatory signaling pathways including the release of IL-1β via the NLRP3 inflammasome
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| ln Vivo |
EVT-401 is currently in clinical development for inflammatory conditions. It has completed Phase I clinical trials in healthy Chinese subjects and is advancing into Phase II studies for moderate to severe active rheumatoid arthritis in patients with inadequate response to methotrexate. The compound demonstrates anti-inflammatory and potential analgesic effects through P2X7 receptor antagonism. In vivo pharmacological data suggest that blocking P2X7 receptors can reduce neuroinflammation and may have therapeutic applications in various inflammatory and pain conditions
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| ADME/Pharmacokinetics |
The study included forced degradation experiments under various stress conditions to evaluate stability, but these were conducted in vitro (acidic hydrolysis, alkaline hydrolysis, oxidation, thermal, photolytic) and not for pharmacokinetic assessment. [1]
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| Toxicity/Toxicokinetics |
The safety and tolerability of EVT-401 have been evaluated in clinical studies. A Phase I study in healthy Chinese subjects was primarily designed to assess the safety profile, tolerability, and dose range of single oral doses of EVT-401 tablets. Multiple-dose safety studies have also been planned to further evaluate the tolerability of the compound. The highest dose tested in single-dose studies has been used to establish safety margins for subsequent clinical trials. Detailed toxicological data including LD50, organ-specific toxicity, and long-term safety profiles are not specified in the available literature.
EVT-401 has been evaluated in clinical pharmacokinetic studies. A Phase I study conducted in healthy Chinese subjects assessed the pharmacokinetic (PK) profile of single oral doses of EVT-401 tablets. Key PK parameters including Cmax, AUC, and elimination half-life have been characterized. The effect of food on the pharmacokinetics of EVT-401 was also investigated. The compound is formulated as an oral tablet. For preclinical animal studies, the compound can be dissolved using formulations such as 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline, which yields a solubility of 2.5 mg/mL. Stock solutions in DMSO can be stored at -80°C for up to 6 months. The study noted that EVT-401 was susceptible to degradation under acidic, alkaline, and oxidative stress conditions, but relatively stable under photolytic and thermal dry stress conditions. [1] |
| References |
[2]. https://pubchem.ncbi.nlm.nih.gov/compound/25013922
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| Additional Infomation |
EVT-401 (2-(3-fluoro-4-(trifluoromethyl)phenyl)-N-(2-(1-hydroxypropan-2-yl)-6-methyl-1-oxo-1,2-dihydroisoquinolin-5-yl)acetamide) is a P2X7 receptor antagonist developed for the treatment of rheumatoid arthritis by preventing disease progression and symptom exacerbation. It has shown efficacy in combating neuroinflammation. Phase I clinical trial of EVT-401 for rheumatoid arthritis has recently been completed. The paper describes the identification and characterization of 14 related substances (6 process-related substances and 8 degradation products) in EVT-401 using LC-MS techniques. EVT-401 was found to be susceptible to acid (1 M HCl, 90°C, 12 h), alkaline (1 M NaOH, 90°C, 8 h), and oxidative (10% H₂O₂, 80°C, 4 h) stress conditions, while relatively stable under photolytic (4500 ± 500 lx, 3 days) and thermal dry (150°C, 5 days) stress conditions. [1]
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| Molecular Formula |
C22H20F4N2O3
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|---|---|
| Molecular Weight |
436.399419784546
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| Exact Mass |
436.1410051
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| CAS # |
951015-69-3
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| PubChem CID |
25013922
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| Appearance |
White to off-white solid powder
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| LogP |
3.4
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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 |
31
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| Complexity |
699
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C1(CC(NC2=C(C)C=CC3=C2C=CN([C@H](C)CO)C3=O)=O)=CC=C(C(F)(F)F)C(F)=C1
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| InChi Key |
JECILOFRRYCNDH-CYBMUJFWSA-N
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| InChi Code |
InChI=1S/C22H20F4N2O3/c1-12-3-5-16-15(7-8-28(21(16)31)13(2)11-29)20(12)27-19(30)10-14-4-6-17(18(23)9-14)22(24,25)26/h3-9,13,29H,10-11H2,1-2H3,(H,27,30)/t13-/m1/s1
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| Chemical Name |
2-[3-fluoro-4-(trifluoromethyl)phenyl]-N-[2-[(2R)-1-hydroxypropan-2-yl]-6-methyl-1-oxoisoquinolin-5-yl]acetamide
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| Synonyms |
EVT-401; EVT401; EVT 401
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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 (229.2 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2915 mL | 11.4574 mL | 22.9148 mL | |
| 5 mM | 0.4583 mL | 2.2915 mL | 4.5830 mL | |
| 10 mM | 0.2291 mL | 1.1457 mL | 2.2915 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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