| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
IRF5-IN-1 targets IRF5 signaling by disrupting IRF5 nuclear translocation without affecting NF-κB p65 activity. It acts through SLC15A4 (a proton-coupled oligopeptide transporter) to selectively inhibit TLR7/8-induced IRF5 responses. This specificity makes it a valuable tool for studying IRF5-mediated inflammatory and autoimmune pathways.
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| ln Vitro |
In vitro, IRF5-IN-1 significantly reduces IRF5 nuclear translocation without affecting the activation of NF-κB p65. It selectively inhibits TLR7/8-induced IRF5 responses in cells. It shows comparable or marginally superior potency to the alternative SLC15A4 inhibitor AJ2-30 in functional pathway inhibition assays.
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| ln Vivo |
In vivo studies for IRF5-IN-1 are limited. As an inhibitor of IRF5 signaling, it has potential for treating autoimmune diseases such as systemic lupus erythematosus. The compound's selectivity for IRF5 over NF-κB suggests a favorable safety profile. Further animal studies are needed to confirm its in vivo efficacy.
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| Enzyme Assay |
Cell-free enzyme assays for IRF5-IN-1: IRF5 DNA binding activity is measured using electrophoretic mobility shift assays (EMSA) or ELISA-based DNA binding assays. Nuclear extracts from treated cells are incubated with IRF5 consensus DNA sequences. Binding is detected by chemiluminescence or fluorescence. SLC15A4 binding can be assessed using surface plasmon resonance or isothermal titration calorimetry.
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| Cell Assay |
Cellular assays for IRF5-IN-1: immune cells (e.g., macrophages or dendritic cells) are treated with IRF5-IN-1 (0.1-50 µM) for 1-24 hours, then stimulated with TLR7/8 agonists. IRF5 nuclear translocation is assessed by immunofluorescence microscopy or subcellular fractionation followed by Western blot. Cytokine production (e.g., IFN-α, TNF-α, IL-6) is measured by ELISA. NF-κB p65 activation is assessed as a control for specificity.
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| Animal Protocol |
In vivo animal studies for IRF5-IN-1: autoimmune mouse models (e.g., lupus-prone MRL/lpr mice) would be used. Animals are administered IRF5-IN-1 orally or intraperitoneally at doses of 10-50 mg/kg for 4-8 weeks. Disease severity, autoantibody levels, and cytokine profiles are assessed. IRF5 nuclear translocation in tissues is evaluated. Tolerability and toxicity are monitored.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of IRF5-IN-1: as a small molecule (molecular weight 431.57), it may have moderate oral bioavailability and tissue distribution. It likely penetrates cells to inhibit IRF5 nuclear translocation. Metabolism and elimination pathways require further investigation. Detailed PK data are limited.
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| Toxicity/Toxicokinetics |
Toxicity of IRF5-IN-1: as a selective IRF5 inhibitor, it may have a favorable safety profile. However, comprehensive toxicity data are limited. The compound is for research use only and not approved for clinical use. Standard laboratory safety precautions should be followed during handling.
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| References | |
| Additional Infomation |
IRF5-IN-1 is a research compound used for studying IRF5 signaling and its role in autoimmune diseases. It is a selective inhibitor that distinguishes IRF5 from NF-κB pathways. It is available as a reference standard for pharmacological studies. No clinical trials or FDA approvals have been reported.
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| Molecular Formula |
C27H33N3O2
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|---|---|
| Molecular Weight |
431.569826841354
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| Exact Mass |
431.257
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| CAS # |
689270-18-6
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| PubChem CID |
5215318
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
5.1
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
32
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| Complexity |
577
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
CJAGKBRBMHETMY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H33N3O2/c1-3-32-22-14-12-21(13-15-22)26-19-24(23-10-4-5-11-25(23)29-26)27(31)28-16-8-18-30-17-7-6-9-20(30)2/h4-5,10-15,19-20H,3,6-9,16-18H2,1-2H3,(H,28,31)
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| Chemical Name |
2-(4-ethoxyphenyl)-N-[3-(2-methylpiperidin-1-yl)propyl]quinoline-4-carboxamide
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.3171 mL | 11.5856 mL | 23.1712 mL | |
| 5 mM | 0.4634 mL | 2.3171 mL | 4.6342 mL | |
| 10 mM | 0.2317 mL | 1.1586 mL | 2.3171 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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