| Size | Price | Stock | Qty |
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| 10mg |
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| 1g | |||
| Other Sizes |
| Targets |
Elubrixin targets CXCR2 (CXC chemokine receptor 2), also known as the IL-8 receptor. As a competitive and reversible antagonist, it binds to CXCR2 and blocks the binding of its ligands, including IL-8 (CXCL8), thereby inhibiting neutrophil chemotaxis and activation. By inhibiting CXCR2, Elubrixin reduces neutrophil CD11b upregulation and shape change, which are key steps in neutrophil activation and recruitment to sites of inflammation.
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| ln Vitro |
Neutrophils are inhibited by elubbrixin in a dose-dependent manner [1].
In vitro, Elubrixin inhibits neutrophil CD11b upregulation with an IC50 of 260.7 nM and neutrophil shape change with an IC50 of 310.5 nM. It inhibits ex vivo neutrophil activation and ozone-induced airway inflammation in humans, demonstrating dose-dependent effects on neutrophil activation and recruitment within a well-tolerated dose range. These activities confirm its potent antagonism of CXCR2-mediated neutrophil functions. |
| ln Vivo |
In vivo, Elubrixin has been investigated for inflammatory diseases such as inflammatory bowel disease and airway inflammation. It inhibits ex vivo neutrophil activation and ozone-induced airway inflammation in humans. The compound's oral activity and efficacy in reducing neutrophil-mediated inflammation support its potential therapeutic application in inflammatory conditions. Clinical studies have evaluated its safety and efficacy in inflammatory diseases.
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| Enzyme Assay |
In vitro receptor binding assays for Elubrixin measure binding to CXCR2 using radioligand binding (e.g., [¹²⁵I]IL-8) in membrane preparations from cells expressing recombinant CXCR2. Competition binding experiments are performed with various concentrations of Elubrixin. IC50 or Ki values are calculated from displacement curves. Functional assays measure inhibition of IL-8-induced calcium flux or chemotaxis in CXCR2-expressing cells.
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| Cell Assay |
Cellular assays for Elubrixin use human neutrophils isolated from whole blood. Neutrophils are treated with various concentrations of Elubrixin. CD11b upregulation is induced by IL-8 or other CXCR2 agonists and measured by flow cytometry using CD11b-specific antibodies. Neutrophil shape change is assessed by light microscopy or flow cytometry (forward scatter). Chemotaxis is measured using Boyden chamber or microfluidic devices.
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| Animal Protocol |
In vivo animal studies for Elubrixin utilize models of inflammatory bowel disease (e.g., DSS-induced colitis, TNBS-induced colitis) and airway inflammation (e.g., ozone-induced airway inflammation, LPS-induced lung inflammation). The compound is administered orally at various doses. Endpoints include inflammatory cell infiltration (neutrophils) in tissues, cytokine levels, histopathology, and disease severity scores. Efficacy is compared to vehicle and reference anti-inflammatory agents.
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| ADME/Pharmacokinetics |
Elubrixin is orally active with favorable pharmacokinetic properties. As a small molecule with molecular weight of 463.3 g/mol, it is orally bioavailable. The compound's pharmacokinetic profile supports once- or twice-daily oral dosing. Detailed PK parameters (half-life, Cmax, AUC, bioavailability) have been characterized in preclinical and clinical studies. Its oral bioavailability is a key feature for development as a therapeutic for chronic inflammatory diseases.
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| Toxicity/Toxicokinetics |
Preclinical toxicity of Elubrixin has been evaluated in standard toxicology studies to support clinical development. As a CXCR2 antagonist, potential adverse effects may include immunosuppression (due to inhibition of neutrophil function), which could increase infection risk. Clinical trials would monitor for infections and other immune-related effects. The compound has shown a well-tolerated safety profile in clinical studies.
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| References |
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| Additional Infomation |
Elubrixin has been used in trials investigating its treatment for cystic fibrosis, colitis, ulcerative colitis, and chronic obstructive pulmonary disease (COPD).
Elubrixin (SB-656933) is a potent, selective, competitive, reversible, and orally active CXCR2/IL-8 receptor antagonist. It inhibits neutrophil CD11b upregulation and shape change with IC50 values of 260.7 nM and 310.5 nM, respectively. It has been investigated for IBD and airway inflammation. It is available for research purposes only. |
| Molecular Formula |
C17H17CL2FN4O4S
|
|---|---|
| Molecular Weight |
463.310683965683
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| Exact Mass |
462.033
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| CAS # |
688763-64-6
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| Related CAS # |
Elubrixin tosylate;960495-43-6;Elubrixin hydrochloride;688763-65-7
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| PubChem CID |
10479502
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
4.51
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| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
29
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| Complexity |
677
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1=CC=C(C(=C1S(N1CCNCC1)(=O)=O)O)NC(NC1C=CC=C(C=1Cl)F)=O
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| InChi Key |
YQYFEGTYCUQBEI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H17Cl2FN4O4S/c18-10-4-5-13(23-17(26)22-12-3-1-2-11(20)14(12)19)15(25)16(10)29(27,28)24-8-6-21-7-9-24/h1-5,21,25H,6-9H2,(H2,22,23,26)
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| Chemical Name |
1-(2-chloro-3-fluorophenyl)-3-(4-chloro-2-hydroxy-3-piperazin-1-ylsulfonylphenyl)urea
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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 | 2.1584 mL | 10.7919 mL | 21.5838 mL | |
| 5 mM | 0.4317 mL | 2.1584 mL | 4.3168 mL | |
| 10 mM | 0.2158 mL | 1.0792 mL | 2.1584 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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