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| Targets |
SX-517 is a non-competitive dual antagonist targeting CXCR1 and CXCR2 (also known as CXCR2/1). CXCR1 and CXCR2 are chemokine receptors that play key roles in neutrophil recruitment and inflammation. By antagonizing both receptors, SX-517 inhibits the inflammatory response mediated by their ligands, CXCL-1 (GRO-α) and CXCL-8 (IL-8).
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| ln Vitro |
Compound 7, SX-517, has an IC50 of 60 nM and effectively inhibits 10 nM CXCL8-induced [35S]GTPγS binding (0.1 nM-0.1 mM; 60 min) [1]. 10 μM; 60 minutes versus Sx-517 In HEK293 cells, HEK293 Sx-517 (10 μM; 0-30 min) stimulates CXCR2-mediated ERK1/2 phosphorylation [1].
SX-517 inhibits CXCL-1-induced Ca²⁺ flux with an IC50 of 38 nM. It antagonizes CXCL-8-induced [³⁵S]GTPγS binding with an IC50 of 60 nM. It suppresses ERK1/2 phosphorylation. The compound demonstrates potent and specific non-competitive dual CXCR1 and CXCR2 antagonism with IC50 values of 38 nM (against CXCL1) and 36 nM (against CXCL8). |
| ln Vivo |
SX-517 demonstrates anti-inflammatory effects in mouse models. Specific in vivo efficacy data and dosing regimens are not extensively detailed in standard reference sources. As a dual CXCR1/2 antagonist, it is expected to inhibit neutrophil recruitment and inflammation in models of acute and chronic inflammatory diseases.
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| Enzyme Assay |
SX-517's receptor binding can be assessed using radioligand binding assays with membrane preparations from cells expressing recombinant human CXCR1 or CXCR2. Competition binding experiments are performed with increasing concentrations of SX-517 against a fixed concentration of a radiolabeled chemokine ligand (e.g., [¹²⁵I]IL-8). Non-specific binding is determined in the presence of an excess of unlabeled ligand. [³⁵S]GTPγS binding assays are used to measure receptor activation and antagonism.
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: HEK293 Cell Tested Concentrations: 10 μM; with or without 100 ng/mL CXCL-8 Incubation Duration: 0, 5, 15, 30 minutes Experimental Results: Complete blockade of CXCL-8 within 30 minutes Induced ERK1/2 phosphorylation. SX-517's cellular activity is evaluated using PMN (polymorphonuclear) cells or cell lines expressing CXCR1 and CXCR2. CXCL-1-induced Ca²⁺ flux is measured using calcium-sensitive fluorescent dyes (e.g., Fluo-4 AM). ERK1/2 phosphorylation is assessed by Western blot using phospho-specific antibodies. The compound's ability to inhibit chemokine-induced cell migration is measured using transwell migration assays. |
| Animal Protocol |
Animal/Disease Models: Male CD1 SWISS mice (10-15 weeks) with dorsal air sacs. SX-517 (Compound 7) (0.2 mg/kg; intravenous (iv) (iv)injection; single dose) Dramatically inhibits receptors in mouse models in vivo [1]. Old) [1]
Doses: 0.02 mg/kg, 0.2 mg/kg Route of Administration: intravenously (iv) (iv)(iv); Single Dose Experimental Results: Cell counts in the pouch of treated animals were Dramatically diminished compared to positive controls. In mouse models of inflammation, SX-517 is administered via intraperitoneal or oral routes. Inflammatory responses are induced by intraperitoneal injection of thioglycollate or by local administration of CXCL-1 or CXCL-8. The recruitment of neutrophils to the peritoneal cavity or to the site of inflammation is measured by flow cytometry or myeloperoxidase (MPO) assay. SX-517's inhibition of neutrophil recruitment and inflammatory cytokine production is assessed. |
| ADME/Pharmacokinetics |
SX-517 has a molecular weight of 382.22 and contains a boronic acid moiety. The compound is soluble in DMSO. Specific pharmacokinetic parameters such as half-life, bioavailability, and plasma protein binding are not extensively detailed in standard reference sources.
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| Toxicity/Toxicokinetics |
The toxicity profile of SX-517 is not extensively documented. As a boronic acid-containing compound, it may have potential for proteasome inhibition or other off-target effects. Specific LD50 values and organ-specific toxicity data are not readily available.
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| References |
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| Additional Infomation |
SX-517 (CAS# 1240494-13-6) is a non-competitive dual antagonist of CXCR1/2 that demonstrates anti-inflammatory effects. It inhibits CXCL-1-induced Ca²⁺ flux (IC50=38 nM), antagonizes CXCL-8-induced [³⁵S]GTPγS binding (IC50=60 nM), and suppresses ERK1/2 phosphorylation. The compound is a research tool for studying chemokine receptor signaling and inflammation.
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| Molecular Formula |
C19H16BFN2O3S
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| Molecular Weight |
382.2164
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| Exact Mass |
382.095
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| CAS # |
1240494-13-6
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| PubChem CID |
46897162
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.663
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| LogP |
3.98
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
27
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| Complexity |
480
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
VZRIHFZJVIOJBE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H16BFN2O3S/c21-15-6-8-16(9-7-15)23-19(24)13-5-10-18(22-11-13)27-12-14-3-1-2-4-17(14)20(25)26/h1-11,25-26H,12H2,(H,23,24)
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| Chemical Name |
[2-[[5-[(4-fluorophenyl)carbamoyl]pyridin-2-yl]sulfanylmethyl]phenyl]boronic acid
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| Synonyms |
SX517 SX 517 SX-517
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ~100 mg/mL (~261.63 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3.75 mg/mL (9.81 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 37.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.54 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6163 mL | 13.0815 mL | 26.1629 mL | |
| 5 mM | 0.5233 mL | 2.6163 mL | 5.2326 mL | |
| 10 mM | 0.2616 mL | 1.3081 mL | 2.6163 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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