SCH 563705
Based on 4 publication(s) in Google Scholar
SCH 563705 is a potent and orally available CXCR2 and CXCR1 antagonist, with IC50s of 1.3 nM, 7.3 nM and Kis of 1 and 3 nM, respectively.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.86%
- CAS. Nr.: 473728-58-4
- Formel: C23H27N3O5
- Molecular Weight:425.48
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) SCH 563705
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Biologische Aktivität
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CXCR2 1 nM (Ki) |
CXCR1 3 nM (Ki) |
CXCR2 1.3 nM (IC50) |
CXCR1 7.3 nM (IC50) |
Mouse CXCR2 5.2 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| CHO | IC50 |
1.3 nM
Compound: 16
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Displacement of [125I]IL8 from human CXCR2 expressed in CHO cells by SPA
Displacement of [125I]IL8 from human CXCR2 expressed in CHO cells by SPA
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[PMID: 17459706] |
| CHO | IC50 |
7.3 nM
Compound: 16
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Displacement of [125I]IL8 from human CXCR1 expressed in CHO cells by SPA
Displacement of [125I]IL8 from human CXCR1 expressed in CHO cells by SPA
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[PMID: 17459706] |
| Neutrophil | IC50 |
0.5 nM
Compound: 16
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Inhibition of GROalpha-induced migration of human neutrophils by chemotaxis assay
Inhibition of GROalpha-induced migration of human neutrophils by chemotaxis assay
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[PMID: 17459706] |
| Neutrophil | IC50 |
37 nM
Compound: 16
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Inhibition of IL8-induced migration of human neutrophils by chemotaxis assay
Inhibition of IL8-induced migration of human neutrophils by chemotaxis assay
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[PMID: 17459706] |
SCH 563705 (Compound 16) is a potent and orally available CXCR2 and CXCR1 antagonist, with IC50s of 1.3 nM, 7.3 nM and Kis of 1 and 3 nM, respectively. SCH 563705 shows potent inhibition against both Gro-a and IL-8 induced human neutrophil migration (chemotaxis IC50 = 0.5 nM, against 30 nM of Gro-a; chemotaxis IC50 = 37 nM, against 3 nM of IL-8)[1]. SCH 563705 potently inhibits mouse CXCR2 (IC50 = 5.2 nM)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 473728-58-4
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Appearance Solid
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Molecular Weight 425.48
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Formel C23H27N3O5
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Color White to off-white
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SMILES
O=C(C(NC1=CC=CC(C(N(C)C)=O)=C1O)=C2N[C@H](CC)C3=CC(C(C)C)=CO3)C2=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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J Allergy Clin Immunol
IL-10 disrupts the Brd4-docking sites to inhibit LPS-induced CXCL8 and TNF-α expression in monocytes: Implications for chronic obstructive pulmonary disease. [Abstract]2015 Sep;136(3):781-791.e9. PMID: 26044852 -
Dev Cell
2018 Nov 19;47(4):409-424.e9. PMID: 30458137 -
Int Immunopharmacol
Genome-wide screen based on 2DG activated NLRP3 inflammasome reveals the priming signal of TLR2/4 to IKKβ but not IKKα. [Abstract]2025 Jan 3:145:113781. PMID: 39657538 -
Mucosal Immunol
Group 3 innate lymphoid cells regulate neutrophil migration and function in human decidua. [Abstract]2016 Nov;9(6):1372-1383. PMID: 26906405
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (235.03 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: ≥ 5 mg/mL (11.75 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (11.75 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
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.
Protokoll
Mice[2]
Induction of anti-collagen antibody-induced arthritis. Anti-collagen antibody-induced arthritis (ABIA) is induced in BALB/c mice (n = 8 mice per treatment group) as follows. On day 0, mice are injected intraperitoneally with 4 mg ArthritoMAB Arthritis-inducing Antibody Cocktail. On day 3, mice are boosted intraperitoneally with 50 μg of lipopolysaccharide from Escherichia coli 055:B5 in 200 μL sterile PBS. In all studies, SCH 563705 is administered in a vehicle consisting of 0.4% METHOCEL E15 premium hydroxypropyl methylcellulose (MC). Clinical scores are determined daily as follows. Each paw is assigned a score of 0-4 based on the following criteria: asymptomatic, 0; slight redness, 1; one or more swollen digits in addition to redness, 2; swelling of entire paw, 3; ankylosing of joints and residing of swelling, 4. The sum of the four paw scores for each mouse (0-16) are plotted against time to calculate the area under the curve (AUC) of disease activity. Paw hickness measurements are made daily using a micrometer caliper over the metatarsals of the paw. The percent change in paw thickness relative to baseline (day 0) measurements is then calculated[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (278 KB)
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SDS (762 KB)
- English - EN (762 KB)
- Français - FR (762 KB)
- Deutsch - DE (762 KB)
- Norwegian - NO (762 KB)
- Español - ES (762 KB)
- Swedish - SV (762 KB)
- Italian - IT (762 KB)
- Korean - KR (762 KB)
- Portuguese - PT (762 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Chao J, et al. C(4)-alkyl substituted furanyl cyclobutenediones as potent, orally bioavailable CXCR2 and CXCR1 receptor antagonists. Bioorg Med Chem Lett. 2007 Jul 1;17(13):3778-83. [Content Brief]
[2]. Min SH, et al. Pharmacological targeting reveals distinct roles for CXCR2/CXCR1 and CCR2 in a mouse model of arthritis. Biochem Biophys Res Commun. 2010 Jan 1;391(1):1080-6. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3503 mL | 11.7514 mL | 23.5029 mL | 58.7572 mL |
| 5 mM | 0.4701 mL | 2.3503 mL | 4.7006 mL | 11.7514 mL | |
| 10 mM | 0.2350 mL | 1.1751 mL | 2.3503 mL | 5.8757 mL | |
| 15 mM | 0.1567 mL | 0.7834 mL | 1.5669 mL | 3.9171 mL | |
| 20 mM | 0.1175 mL | 0.5876 mL | 1.1751 mL | 2.9379 mL | |
| 25 mM | 0.0940 mL | 0.4701 mL | 0.9401 mL | 2.3503 mL | |
| 30 mM | 0.0783 mL | 0.3917 mL | 0.7834 mL | 1.9586 mL | |
| 40 mM | 0.0588 mL | 0.2938 mL | 0.5876 mL | 1.4689 mL | |
| 50 mM | 0.0470 mL | 0.2350 mL | 0.4701 mL | 1.1751 mL | |
| 60 mM | 0.0392 mL | 0.1959 mL | 0.3917 mL | 0.9793 mL | |
| 80 mM | 0.0294 mL | 0.1469 mL | 0.2938 mL | 0.7345 mL | |
| 100 mM | 0.0235 mL | 0.1175 mL | 0.2350 mL | 0.5876 mL |
SCH 563705 Related Classifications
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