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

CXCR2-IN-2 

Cat. No.: HY-120878 Purity: 99.35% ee.: 98.82%
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

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 440 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 440 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 400 In-stock
Estimated Time of Arrival: December 31
10 mg USD 680 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1350 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2200 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3400 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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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.
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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 240 mg/mL (578.45 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4102 mL 12.0511 mL 24.1022 mL
5 mM 0.4820 mL 2.4102 mL 4.8204 mL
10 mM 0.2410 mL 1.2051 mL 2.4102 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 6 mg/mL (14.46 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.35% ee.: 98.82%

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Keywords:

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

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