1. GPCR/G Protein
    Immunology/Inflammation
  2. CXCR
  3. CXCR2-IN-2

CXCR2-IN-2 

Cat. No.: HY-120878
Handling Instructions

CXCR2-IN-2 is a selective, brain penetrant, and orally bioavailable CXCR2 antagonist (IC50=5.2 nM/1 nM in β-arrestin assay/CXCR2 Tango assay, respectively). CXCR2-IN-2 displays ~730-fold selectivity over CXCR1 and >1900-fold selectivity over all other chemokine receptors. CXCR2-IN-2 inhibits human whole blood Gro-α induced CD11b expression with an IC50 of 0.04 μM.

For research use only. We do not sell to patients.

CXCR2-IN-2 Chemical Structure

CXCR2-IN-2 Chemical Structure

CAS No. : 1838123-21-9

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Description

CXCR2-IN-2 is a selective, brain penetrant, and orally bioavailable CXCR2 antagonist (IC50=5.2 nM/1 nM in β-arrestin assay/CXCR2 Tango assay, respectively). CXCR2-IN-2 displays ~730-fold selectivity over CXCR1 and >1900-fold selectivity over all other chemokine receptors. CXCR2-IN-2 inhibits human whole blood Gro-α induced CD11b expression with an IC50 of 0.04 μM[1].

IC50 & Target[1]

CXCR2

5.2 nM (IC50)

CXCR1

3.8 μM (IC50)

In Vivo

CXCR2-IN-2 (compound 68) (1-10 mg/kg; p.o.; twice daily for 3 days) dose-dependently reduces neutrophil infiltration in vivo in rat and mouse air pouch models[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 6-8 week old male C57Bl/6 mice (Air Pouch Model in Mouse)[1]
Dosage: 1, 3, and 10 mg/kg
Administration: P.o.; twice daily for 3 days
Result: Significantly inhibited neutrophil infiltration into mouse air pouch.
Animal Model: 8-10 week old male Wistar rats (Air Pouch Model in Rat)[1]
Dosage: 1, 3, and 10 mg/kg
Administration: P.o.; twice daily for 3 days
Result: Inhibited neutrophil migration to air pouch in rat.
Molecular Weight

414.90

Formula

C₁₈H₂₃ClN₂O₅S

CAS No.

1838123-21-9

SMILES

O=C(N[[email protected]]1C(C)=CCC1)NC2=CC=C(Cl)C(S(=O)([[email protected]]3(C)COCC3)=O)=C2O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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Keywords:

CXCR2-IN-2CXCRCXC chemokine receptorsC-X-C motif chemokine receptorsneutrophilairpouchC57Bl/6micewholebloodbrainpenetrantoralInhibitorinhibitorinhibit

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CXCR2-IN-2
Cat. No.:
HY-120878
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