CXCR2 antagonist 10
CXCR2 antagonist 10 (Compound 10b) is a CCR2 antagonist with an IC50 of 0.48 μM. CXCR2 antagonist 10 also exhibits antagonistic activity against CXCR2/CCR7, with IC50 values of 4.18 μM and 2.07 μM, respectively. CXCR2 antagonist 10 is applicable for cancer research.
For research use only. We do not sell to patients.
- Formula: C15H15F3N6OS
- Molecular Weight:384.38
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
CCR2 0.48 μM () |
CCR7 2.07 μM () |
CXCR2 4.18 μM () |
Parmacokinetics
| Species | Dose | Route | Cmax | AUC0-last | CL | Vz | T1/2 | Tmax | Bioavailability |
|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 1 mg/kg | i.v. | 3154 ng/mL | 3487 ng·h/mL | 286 mL/h/kg | 504 mL/kg | 1.2 h | / | / |
| Rat[1] | 1 mg/kg | i.v. | 3154 ng/mL | 3487 ng·h/mL | 286 mL/h/kg | 504 mL/kg | 1.2 h | / | / |
| Rat[1] | 5 mg/kg | i.g. | 3920 ng/mL | 28867 ng·h/mL | / | / | 2.16 h | 0.25 h | 165 % |
| Rat[1] | 5 mg/kg | i.g. | 3920 ng/mL | 28867 ng·h/mL | / | / | 2.16 h | 0.25 h | 165 % |
Chemical Information
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Molecular Weight 384.38
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Formula C15H15F3N6OS
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SMILES
OC[C@@H](C)NC1=NC(SCC2=CC=C(C(F)(F)F)C=C2)=NC3=C1N=NN3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)