| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
Purity: ≥98%
| Targets |
CXCR2 is a G protein-coupled receptor for ELR+ CXC chemokines including IL-8, which mediates neutrophil chemotaxis and activation. By blocking CXCR2, Elubrixin inhibits neutrophil recruitment to sites of inflammation, reducing tissue damage. It is a potent and selective CXCR2 antagonist with an IC50 of 2.5 nM.
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|---|---|
| ln Vitro |
In vitro, Elubrixin inhibits CXCR2-mediated neutrophil chemotaxis and activation with an IC50 of 2.5 nM. It blocks IL-8-induced calcium mobilization and CD11b upregulation in neutrophils. Elubrixin shows selectivity for CXCR2 over other chemokine receptors.
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| ln Vivo |
In vivo, Elubrixin inhibits neutrophil recruitment in animal models of inflammation. It is developed for COPD and cystic fibrosis. Elubrixin reduces airway inflammation and neutrophil infiltration. It is orally active and has potential for treating neutrophil-driven inflammatory diseases.
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| Enzyme Assay |
CXCR2 binding assays use membranes from cells expressing recombinant CXCR2 and radiolabeled IL-8 or a CXCR2 antagonist. Elubrixin is serially diluted and incubated with membranes. Bound radioactivity is measured by rapid filtration. IC50 values are determined from competition curves.
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| Cell Assay |
For neutrophil chemotaxis assays, human neutrophils are isolated and placed in Boyden chambers with IL-8 as chemoattractant. Elubrixin is added, and migrated cells are counted. CD11b upregulation is measured by flow cytometry.
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| Animal Protocol |
Animal models include LPS-induced lung inflammation in mice or rats. Elubrixin is administered orally or intranasally. Neutrophil infiltration in bronchoalveolar lavage fluid is measured by flow cytometry or myeloperoxidase assay.
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| References |
Kaur M, Singh D. Neutrophil chemotaxis caused by chronic obstructive pulmonary disease alveolar macrophages: the role of CXCL8 and the receptors CXCR1/CXCR2. J Pharmacol Exp Ther. 2013 Oct;347(1):173-80. doi: 10.1124/jpet.112.201855. Epub 2013 Aug 2. PubMed PMID: 23912333.
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| Molecular Formula |
C17H18CL3FN4O4S
|
|---|---|
| Exact Mass |
498.009
|
| CAS # |
688763-65-7
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| Related CAS # |
Elubrixin tosylate;960495-43-6;Elubrixin;688763-64-6
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| PubChem CID |
23661207
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| Appearance |
Typically exists as solid at room temperature
|
| Hydrogen Bond Donor Count |
5
|
| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
|
| Heavy Atom Count |
30
|
| Complexity |
677
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(NC1=CC=C(C(S(=O)(N2CCNCC2)=O)=C1O)Cl)NC3=C(Cl)C(F)=CC=C3.Cl
|
| InChi Key |
1-(2-Chloro-3-fluorophenyl)-3-(4-chloro-2-hydroxy-3-piperazin-1-ylsulfonylphenyl)urea hydrochloride
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| InChi Code |
AYSVMKUSGQQRHL-UHFFFAOYSA-N
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| Chemical Name |
SB-656933 SB 656933 SB656933 SB-656933-AAF SB-656933 AAF SB-656933AAF Elubrixin Elubrixin HCl Elubrixin hydrochloride
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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.) |
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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