SX-517
Based on 1 Customer Validation
SX-517 is a dual CXCR2/1 antagonist, containing boronic acid. SX-517 inhibits CXCL1-induced Ca2+ flux (IC50=38 nM), and antagonizes CXCL8-induced [(35)S]GTPγS binding (IC50=60 nM) and ERK1/2 phosphorylation. SX-517 has significant ability for inflammation suppression, in both humanized polymorphonuclear (PMN) cells and in murine model.
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- Purity: 99.90%
- CAS No.: 1240494-13-6
- 화학식: C19H16BFN2O3S
- 분자량:382.22
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보관:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
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CXCR2 |
CXCR1 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
210 nM
Compound: 7, SX-517
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Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced intracellular Ca2+ release by fluorescence based calcium flux assay
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced intracellular Ca2+ release by fluorescence based calcium flux assay
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[PMID: 25254640] |
| HEK293 | IC50 |
60 nM
Compound: 7, SX-517
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Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CVCL8-induced [35S]GTPgammaS binding after 60 mins
Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CVCL8-induced [35S]GTPgammaS binding after 60 mins
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[PMID: 25254640] |
| HEK293 | IC50 |
880 nM
Compound: 7, SX-517
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Antagonist activity at human CXCR1 expressed in HEK293 cells assessed as inhibition of CXCL8-induced intracellular Ca2+ release by fluorescence based calcium flux assay
Antagonist activity at human CXCR1 expressed in HEK293 cells assessed as inhibition of CXCL8-induced intracellular Ca2+ release by fluorescence based calcium flux assay
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[PMID: 25254640] |
SX-517 (compound 7) (0.1 nM-0.1 mM; 60 min) potently inhibits [35S]GTPγS binding induced by 10 nM CXCL8 with an IC50 of 60 nM[1].
SX-517 (10 μM; 60 min) has inhibitory effect on the cell surface expression of CXCR2 in HEK293 cells[1].
SX-517 (10 μM; 0-30 min) blocks CXCR2-mediated phosphorylation of ERK1/2 in HEK293 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293 cells
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Concentration:10 μM; with or without 100 ng/mL CXCL-8
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Incubation Time:0, 5, 15, 30 min
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Result:Completely blocked CXCL-8-induced phosphorylation of ERK1/2 by 30 min.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male CD1 SWISS mice with an air-pouch on the backs (10-15 week old)[1]
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Dosage:0.02 mg/kg, 0.2 mg/kg
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Administration:Intravenous injection; single dose
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Result:Significant reduction in cell count in the pouches of treated animals compared to the positive control cohort.
Chemical Information
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CAS No. 1240494-13-6
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Appearance Solid
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분자량 382.22
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화학식 C19H16BFN2O3S
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Color White to off-white
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SMILES
OB(C1=CC=CC=C1CSC2=NC=C(C(NC3=CC=C(F)C=C3)=O)C=C2)O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
용액&용해도
DMSO : 100 mg/mL (261.63 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.54 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. 2-[5-(4-Fluorophenylcarbamoyl)pyridin-2-ylsulfanylmethyl]phenylboronic Acid (SX-517): Noncompetitive Boronic Acid Antagonist of CXCR1 and CXCR2. J Med Chem. 2014 Oct 23;57(20):8378-97. [Content Brief]
[2]. Ti H, et al. Targeted Treatments for Chronic Obstructive Pulmonary Disease (COPD) Using Low-Molecular-Weight Drugs (LMWDs). J Med Chem. 2019 Jul 11;62(13):5944-5978. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6163 mL | 13.0815 mL | 26.1629 mL | 65.4074 mL |
| 5 mM | 0.5233 mL | 2.6163 mL | 5.2326 mL | 13.0815 mL | |
| 10 mM | 0.2616 mL | 1.3081 mL | 2.6163 mL | 6.5407 mL | |
| 15 mM | 0.1744 mL | 0.8721 mL | 1.7442 mL | 4.3605 mL | |
| 20 mM | 0.1308 mL | 0.6541 mL | 1.3081 mL | 3.2704 mL | |
| 25 mM | 0.1047 mL | 0.5233 mL | 1.0465 mL | 2.6163 mL | |
| 30 mM | 0.0872 mL | 0.4360 mL | 0.8721 mL | 2.1802 mL | |
| 40 mM | 0.0654 mL | 0.3270 mL | 0.6541 mL | 1.6352 mL | |
| 50 mM | 0.0523 mL | 0.2616 mL | 0.5233 mL | 1.3081 mL | |
| 60 mM | 0.0436 mL | 0.2180 mL | 0.4360 mL | 1.0901 mL | |
| 80 mM | 0.0327 mL | 0.1635 mL | 0.3270 mL | 0.8176 mL | |
| 100 mM | 0.0262 mL | 0.1308 mL | 0.2616 mL | 0.6541 mL |
SX-517 Related Classifications
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