| Size | Price | Stock | Qty |
|---|---|---|---|
| 25mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| 500mg | |||
| Other Sizes |
| Targets |
IRAK4 (Interleukin-1 receptor-associated kinase 4)
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|---|---|
| ln Vitro |
IRAK4 inhibitor-1 is a potent inhibitor of IRAK4, the most upstream kinase in the Toll/Interleukin-1 receptor (TIR) signaling pathway. IRAK4 is a key mediator of innate immune signaling, phosphorylating downstream targets including IRAK1 and leading to activation of NF-κB and MAPK pathways. Inhibition of IRAK4 blocks the production of pro-inflammatory cytokines such as TNFα, IL-1β, and IL-6. The compound's potency and selectivity for IRAK4 make it a valuable tool for studying innate immune signaling.
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| ln Vivo |
In vivo studies of IRAK4 inhibitors demonstrate efficacy in animal models of inflammatory diseases, autoimmune disorders, and cancer. IRAK4 inhibition reduces pro-inflammatory cytokine production and ameliorates disease severity in models of rheumatoid arthritis, inflammatory bowel disease, and other inflammatory conditions. The compound's ability to modulate the TIR signaling pathway makes it a promising therapeutic candidate.
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| Enzyme Assay |
IRAK4 kinase activity is measured using radiometric or fluorescence-based kinase assays with recombinant IRAK4 enzyme and appropriate substrates. IC50 values are determined from dose-response curves. Selectivity profiling is conducted against other kinases to confirm specificity for IRAK4.
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| Cell Assay |
Cellular potency is evaluated in immune cells by measuring IRAK4-mediated signaling. Cells are stimulated with IL-1 or Toll-like receptor agonists, and IRAK4-dependent phosphorylation of downstream targets is measured by Western blot. Pro-inflammatory cytokine production is measured by ELISA to assess the functional impact of IRAK4 inhibition.
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| Animal Protocol |
In vivo efficacy is evaluated in animal models of inflammatory and autoimmune diseases. IRAK4 inhibitor-1 is administered via appropriate routes at various doses. Disease severity, inflammatory markers, and cytokine levels are assessed. Pharmacodynamic biomarkers are measured to confirm target engagement and pathway modulation.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for IRAK4 inhibitor-1 are limited as the compound is primarily used as a research tool. The compound has a molecular weight of 491.50. Detailed PK parameters such as half-life, clearance, and bioavailability are available from preclinical studies.
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| Toxicity/Toxicokinetics |
Comprehensive toxicological data for IRAK4 inhibitor-1 are limited as the compound is primarily used for research purposes. Standard laboratory safety precautions should be observed during handling. The compound is not intended for human therapeutic use and has not been evaluated in formal toxicology studies.
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| Additional Infomation |
IRAK4 inhibitor-1 is a research tool for studying IRAK4 function in innate immune signaling. IRAK4 is the most upstream kinase in the Toll/Interleukin-1 receptor (TIR) signaling pathway and plays a critical role in mediating inflammatory responses. IRAK4 inhibitors are being explored as therapeutic agents for inflammatory diseases, autoimmune disorders, and certain cancers. The compound was first described in patent WO 2015104688.
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| Molecular Formula |
C24H25N7O5
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|---|---|
| Molecular Weight |
491.499204397202
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| Exact Mass |
491.19
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| Elemental Analysis |
C, 58.65; H, 5.13; N, 19.95; O, 16.28
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| CAS # |
1801344-12-6
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| PubChem CID |
122700070
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| Appearance |
Solid powder
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| LogP |
1.7
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
36
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| Complexity |
773
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC1=NC=CC(=C1)C2=NC(=CO2)C(=O)NC3=CC4=C(N=C3N5CC[C@@H](C5)O)N=C(O4)N6CCOCC6
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| InChi Key |
SJHNWSAWWOAWJH-INIZCTEOSA-N
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| InChi Code |
InChI=1S/C24H25N7O5/c1-14-10-15(2-4-25-14)23-27-18(13-35-23)22(33)26-17-11-19-20(28-21(17)31-5-3-16(32)12-31)29-24(36-19)30-6-8-34-9-7-30/h2,4,10-11,13,16,32H,3,5-9,12H2,1H3,(H,26,33)/t16-/m0/s1
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| Chemical Name |
N-[5-[(3S)-3-hydroxypyrrolidin-1-yl]-2-morpholin-4-yl-[1,3]oxazolo[4,5-b]pyridin-6-yl]-2-(2-methylpyridin-4-yl)-1,3-oxazole-4-carboxamide
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| Synonyms |
SIN44126; SIN-44126; SIN 44126; CAS-4948; CAS4948; CAS 4948;
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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 | 2.0346 mL | 10.1729 mL | 20.3459 mL | |
| 5 mM | 0.4069 mL | 2.0346 mL | 4.0692 mL | |
| 10 mM | 0.2035 mL | 1.0173 mL | 2.0346 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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