(R,R)-CXCR2-IN-2, a diastereoisomer of CXCR2-IN-2 (compound 68), functions as a brain-penetrant CXCR2 antagonist. It exhibits a pIC50 of 9 in the Tango assay and 6.8 in the HWB Gro-α induced CD11b expression assay[1].

CXCR2-IN-2 is a selective CXCR2 antagonist that is brain penetrant and orally bioavailable, with IC50 values of 5.2 nM and 1 nM in the β-arrestin assay and CXCR2 Tango assay, respectively. It exhibits approximately 730-fold selectivity over CXCR1 and greater than 1900-fold selectivity over all other chemokine receptors. Furthermore, CXCR2-IN-2 effectively inhibits Gro-α induced CD11b expression in human whole blood, displaying an IC50 of 0.04 μM[1].

CXCR2-IN-1 has a pIC50 of 9.3 and is a CXCR2 antagonist of the central nervous system penetration agent.

Navarixin (MK-7123)(SCH527123) is a novel, selective CXC chemokine receptor 2(CXCR2) antagonist that inhibits neutrophil activation and modulates neutrophil trafficking in animal models, characteristics that may be beneficial in the treatment of conditions with unbalanced pulmonary neutrophilia.

AZD8797 (KAND567) is an orally available, selective and potent human CX3CR1-converting antagonist with inhibitory effects on CX3CR1 and CXCR2, and potentially protects against SARS-CoV-2-induced neuronal damage, preventing worsening of nociceptive sensitization and microglial activation in a migraine model of rats following seizures.

Corydalmine hydrochloride is a chemical compound that suppresses spore germination in certain plant pathogenic and saprophytic fungi [1], serves as an effective oral analgesic agent with potent activity [2], and mitigates Vincristine-induced neuropathic pain in mice through the inhibition of an NF-κB-dependent CXCL1/CXCR2 signaling pathway [3].

CXCR2 antagonist 3 (compound 11h) is a highly effective antagonist of CXC chemokine receptor 2 (CXCR2). It displays potent activity in inhibiting neutrophil infiltration into the air pouch, with double-digit nanomolar potencies against CXCR2. Moreover, CXCR2 antagonist 3 reduces the infiltration of neutrophils and MDSCs, while enhancing the infiltration of CD3+ T lymphocytes into Pan02 tumor tissues [1].