CXCR2-IN-2

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].

Product Specifications

CAS Number

[1838123-21-9]

UNSPSC

12352005

Target

CXCR

Type

Reference compound

Related Pathways

GPCR/G Protein; Immunology/Inflammation

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/cxcr2-in-2.html

Purity

99.52

Solubility

DMSO : 240 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C18H23ClN2O5S

Molecular Weight

414.90

References & Citations

[1]Lu H, et al. Discovery of Novel 1-Cyclopentenyl-3-phenylureas as Selective, Brain Penetrant, and Orally Bioavailable CXCR2 Antagonists. J Med Chem. 2018;61 (6) :2518-2532.