1. GPCR/G Protein Immunology/Inflammation
  2. CCR CXCR
  3. 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.

CXCR2 antagonist 10

CXCR2 antagonist 10 Chemical Structure

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Description

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[1].

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 %
Molecular Weight

384.38

Formula

C15H15F3N6OS

SMILES

OC[C@@H](C)NC1=NC(SCC2=CC=C(C(F)(F)F)C=C2)=NC3=C1N=NN3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
CXCR2 antagonist 10
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HY-181681
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