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SX-517 is a novel and potent boronic acid-based dual CXCR1/2 antagonist, acting noncompetitively with IC50 of 38 nM (vs. CXCL1) and 36 nM (vs. CXCL8), respectively. It has anti-inflammatory effects in an in vivo murine model (0.2 mg/kg iv).
| 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].
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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. |
| 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. |
| References |
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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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