| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
EJMC-1 targets the pro-inflammatory cytokine Tumor Necrosis Factor-alpha (TNF-α). By inhibiting TNF-α, it reduces the downstream inflammatory cascade that is implicated in various diseases, including rheumatoid arthritis, inflammatory bowel disease, and psoriasis. In an in vitro competitive binding assay, EJMC-1 inhibits the binding of recombinant human TNFα to TNF receptor 1-ECD by 28.0%.
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|---|---|
| ln Vitro |
In vitro, EJMC-1 inhibits TNF-α with an IC50 of 42 μM. In HEK293T cells transfected with specific plasmids, it demonstrates inhibitory activity against TNFα with an IC50 of 42300.0 nM, as measured by the Dual-glo luciferase assay system. Additionally, it inhibits TNFα-induced IkappaB-alpha phosphorylation in HeLa cells with an IC50 of 45700.0 nM, as assessed by ELISA after 15 minutes.
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| ln Vivo |
In vivo activity data for EJMC-1 are not detailed in the available literature. Its characterization is primarily based on its in vitro TNF-α inhibitory activity.
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| Enzyme Assay |
Non-cellular assays for EJMC-1 typically involve measuring its inhibition of TNF-α activity. In a typical assay, the compound is incubated with TNF-α and a TNF-α-sensitive reporter cell line or with purified TNF-α and its receptor. The inhibition of TNF-α-induced signaling or binding is measured, and the IC50 is calculated.
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| Cell Assay |
In vitro cellular assays for EJMC-1 are not standardly described. Its activity is primarily characterized in non-cellular or cell-free systems to measure direct TNF-α inhibition.
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| Animal Protocol |
In vivo animal studies for EJMC-1 are not detailed. Based on its TNF-α inhibitory mechanism, it could potentially be evaluated in animal models of inflammatory diseases, but such studies are not documented.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of EJMC-1 are not extensively characterized. As a small molecule with a molecular weight of 374.80, it is soluble in DMSO (100 mg/mL).
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| Toxicity/Toxicokinetics |
Specific toxicological data for EJMC-1 are limited. As a research compound, comprehensive toxicity profiles are not available. It is intended for research use only and not for human therapeutic use.
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| References | |
| Additional Infomation |
EJMC-1 is a research-grade compound for laboratory use only and is not approved for clinical use. Its primary application is in inflammation research to study the role of TNF-α in various diseases and to evaluate the potential of TNF-α inhibitors as therapeutic agents.
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| Molecular Formula |
C17H11CLN2O4S
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|---|---|
| Molecular Weight |
374.7982
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| Exact Mass |
374.012
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| CAS # |
397281-20-8
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| PubChem CID |
1367407
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.651±0.06 g/cm3(Predicted)
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| LogP |
2.9
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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 |
25
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| Complexity |
637
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC2=C(C=CC3=C2C(=C1)C(=O)N3)S(=O)(=O)NC4=CC(=C(C=C4)O)Cl
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| InChi Key |
FQWAQUPLBBOCSP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H11ClN2O4S/c18-12-8-9(4-6-14(12)21)20-25(23,24)15-7-5-13-16-10(15)2-1-3-11(16)17(22)19-13/h1-8,20-21H,(H,19,22)
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| Chemical Name |
N-(3-chloro-4-hydroxyphenyl)-2-oxo-1H-benzo[cd]indole-6-sulfonamide
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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 : ~125 mg/mL (~333.51 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 | 2.6681 mL | 13.3404 mL | 26.6809 mL | |
| 5 mM | 0.5336 mL | 2.6681 mL | 5.3362 mL | |
| 10 mM | 0.2668 mL | 1.3340 mL | 2.6681 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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