CXCR2 Antagonist

SB225002, a potent, selective and non-peptide CXCR2 antagonist, inhibits ¹²⁵I-IL-8 binding to CXCR2 with an IC₅₀ of 22 nM.

Navarixin (SCH 527123) is a potent, allosteric and orally active antagonist of both CXCR1 and CXCR2, with K_d values of 41 nM for cynomolgus CXCR1 and 0.20 nM, 0.20 nM, 0.08 nM for mouse, rat and cynomolgus monkey CXCR2, respectivelly.

AZD-5069 is a potent CXCR2 chemokine receptor antagonist, used for caner treatment.

NVP CXCR2 20 is a selective CXCR2 inhibitor with analgesic and antinociceptive activities. NVP CXCR2 20 selectively blocks CXCR2 signaling and attenuates mechanical and thermal hypersensitivity in rat chronic constriction injury (CCI) models. NVP CXCR2 20 inhibits CXCL3-induced hypersensitivity in naive mice and reduces elevated CXCL3 protein levels in the spinal cord and dorsal root ganglia (DRG) of CCI-exposed rats. NVP CXCR2 20 can be used for the research of neuropathic pain and chronic obstructive pulmonary disease (COPD).

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.

SB-265610 is a selective, competitive, nonpeptide and allosteric CXCR2 antagonist. SB-265610 blocks rat cytokine-induced neutrophil chemoattractant-1 (CINC-1)-induced calcium mobilization and neutrophil chemotaxis with IC₅₀s of 3.7 nM and 70 nM, respectively.

Cosalane (NSC 658586) is a CCR7 (IC₅₀ = 2.43 μM) and CXCR2 antagonist (IC₅₀ = 0.66 μM). Cosalane is an inhibitor of HIV replication with a wide range of activity against HIV-1 isolates, HIV-2, Rauscher murine leukemia virus, HSV-1, HSV-2 and human cytomegalovirus. Cosalane inhibits both attachment of gp120 to CD4. Cosalane inhibits human and murine CCR7 in response to both CCL19 and CCL21 agonists. Cosalane can be studied in research for HIV or attenuating acute graft-versus-host disease (aGVHD) in allogeneic hematopoietic stem cell transplantation (HSCT).

Nicotinamide N-oxide, an in vivo nicotinamide metabolite, is a potent, and selective antagonist of the CXCR2 receptor.

Danirixin is a selective, and reversible CXCR2 antagonist, with IC₅₀?of?12.5 nM for CXCL8.

SX-517 is a dual CXCR2/1 antagonist, containing boronic acid. SX-517 inhibits CXCL1-induced Ca²⁺ flux (IC₅₀=38 nM), and antagonizes CXCL8-induced [(35)S]GTPγS binding (IC₅₀=60 nM) and ERK1/2 phosphorylation. SX-517 has significant ability for inflammation suppression, in both humanized polymorphonuclear (PMN) cells and in murine model.

Ladarixin sodium (DF 2156A) is an orally active, allosteric non-competitive and dual CXCR1 and CXCR2 antagonist. Ladarixin sodium can be used for the research of COPD and asthma.

Elubrixin tosylate (SB-656933 tosylate) is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist. Elubrixin tosylate inhibits neutrophil CD11b upregulation (IC₅₀ of 260.7 nM) and shape change (IC₅₀ of 310.5 nM). Elubrixin tosylate has the potential for inflammatory diseases research, such as inflammatory bowel disease and airway inflammation.

SCH 563705 is a potent and orally available CXCR2 and CXCR1 antagonist, with IC₅₀s of 1.3 nM, 7.3 nM and K_is of 1 and 3 nM, respectively.

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.

SRT3109 is an antagonist of CXCR2, with a pIC₅₀ of 8.2, and used in the research of chemokine mediated diseases.

AZD8309 is an orally active antagonist of CXCR2. AZD8309 has the ability to regulate the transmigration of neutrophils. AZD8309 can be used in the study of inflammatory diseases.

CXCR2 antagonist 8 is a potent and selective CXCR2 antagonist. CXCR2 antagonist 8 can be used for insulin resistance research.

Elubrixin (SB-656933) is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist. Elubrixin inhibits neutrophil CD11b upregulation (IC₅₀ of 260.7 nM) and shape change (IC₅₀ of 310.5 nM). Elubrixin has the potential for inflammatory diseases research, such as inflammatory bowel disease and airway inflammation.

SRT3190 is an antagonist of CXCR2, used in the research of chemokine mediated diseases.

Nicotinamide N-oxide (Standard) is the analytical standard of Nicotinamide N-oxide. This product is intended for research and analytical applications. Nicotinamide N-oxide, an in vivo nicotinamide metabolite, is a potent, and selective antagonist of the CXCR2 receptor.