CXCR Antagonist

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

UNBS5162 is a pan-antagonist of CXCL chemokine expression, with anti-tumor activity.

SB-332235 is a potent, orally active nonpeptide CXCR2 antagonist, with an IC₅₀ of 7.7 nM. SB-332235 displays 285-fold selectivity for CXCR2 over CXCR1. SB-332235 inhibits acute and chronic models of arthritis in the rabbit. SB-332235 inhibits viability of AML cells.

Vimnerixin (AZD4721) is the potent and orally active antagonist of acidic CXC chemokine receptor 2 (CXCR2). Vimnerixin has the potential for the research of inflammatory disease.

CXCR2 antagonist 2 is a potent CXCR2 antagonist for cancer immunoresearch with an IC₅₀ value of 95 nM.

DV1 TFA is a CXCR4 inhibitor with anti-proteolytic properties that specifically blocks the binding of SDF-1α to its receptor. DV1 TFA inhibits the migration of breast cancer cells and enables the targeted delivery of avidin-PLGA nanoparticles to CXCR4-expressing cancer cells. DV1 TFA not only effectively suppresses the progression of metastatic breast cancer in mouse models, but also preferentially accumulates in brain tumor tissues rather than normal brain tissues, showing potential for inhibiting intracranial tumor metastasis. As a humoral immune stimulant, DV1 TFA induces the production of specific IgG, neutralizing antibodies and cellular immune responses, thereby providing the host with protection against lethal challenges. DV1 TFA has been applied to studies on CXCR4-expressing cancers, glioblastoma, dengue fever and other related diseases.

EMU-116 is an orally active CXCR4 antagonist. EMU-116 can be used in the study of cancer.

(±)-NBI-74330 is a potent and selective CXCR3 antagonist. (±)-NBI-74330 not only reduces tactile and thermal hypersensitivity but also enhances the analgesic properties of morphine. (±)-NBI-74330 can reduce microglial cell activation, increase astroglial cell activation, and downregulate the expression of some CXCR3 ligands in a rat neuropathic pain model.

(R,R)-CXCR2-IN-2 (compound 67), diastereoisomer of CXCR2-IN-2 (compound 68) (HY-120878), is a CXCR2 antagonist with a pIC₅₀ of 9 and 6.8 in the Tango assay and d in the HWB Gro-α induced CD11b expression assay, respectively.

(S)-SCH 563705 is a S-enantiomer of SCH 563705. SCH 563705 (compound 16) 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.

PF-06835375 is a selective, humanized CXCR5-targeting immunoglobulin G1 antibody. PF-06835375 depletes CXCR5-positive B cells, follicular helper T cells and circulating Tfh-like cells. PF-06835375 is applicable to research related to autoimmune diseases.

(Rac)-SCH 563705 is a racemic mixture of SCH 563705 (HY-10011). SCH 563705 (compound 16) is a potent and orally active CXCR2 and CXCR1 antagonist with IC₅₀ values ​​of 1.3 nM and 7.3 nM and K_i values ​​of 1 nM and 3 nM, respectively.

HF51116 is a potent antagonist of CXCR4. HF51116 strongly antagonizes SDF-1α-induced cell migration, calcium mobilization, and CXCR4 internalization. HF51116 inhibits HIV-1 infection via CXCR4. HF51116 has the potential for the research of HIV-1 infection, hematopoietic stem cell mobilization, and cancer metastasis.

Plerixafor-d₄ is the deuterium labeled Plerixafor. Plerixafor (AMD 3100) is a selective CXCR4 antagonist with an IC₅₀ of 44 nM. Plerixafor, an immunostimulant and a hematopoietic stem cell (HSC) mobilizer, is an allosteric agonist of CXCR7. Plerixafor inhibits HIV-1 and HIV-2 replication with an EC₅₀ of 1-10 nM.

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

CXCR2/CCR7 antagonist-1 (compound 6) is a potent CXCR2 and CCR7 dual antagonist with IC₅₀s of 0.0046 and 0.0014 μM, respectively. CXCR2/CCR7 antagonist-1 can be used in the study of cancer metastasis and autoimmune diseases.

VUF5834 is a non-peptide chemokine receptor CXCR3 antagonist with non-competitive antagonistic and inverse agonistic activities. VUF5834 blocks the effects of CXCL10 and CXCL11 on human CXCR3, exhibits non-competitive antagonistic and inverse agonistic properties to CXCR3, and, except for TAK-779, has a slightly lower affinity for rodent CXCR3 than for primate CXCR3.

Peptide E5 is an antagonist targeting the CXCR4/CXCL12 axis. Peptide E5 blocks the CXCR4/CXCL12 axis, downregulates CXCR4 expression, and inhibits the phosphorylation of downstream Akt and Erk. Peptide E5 induces apoptosis, suppresses migration and adhesion of breast cancer cells. Peptide E5 inhibits CXCL12-mediated endothelial progenitor cell recruitment, thereby suppressing tumor angiogenesis. Peptide E5 is applicable to relevant research on breast cancer.

AMD 3465 (Standard) is the analytical standard of AMD 3465. This product is intended for research and analytical applications. AMD 3465 (GENZ-644494) is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells; AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM), but has no effect on CCR5-using (R5) viruses.

ACT-672125 is a potent CXCR3 antagonist with IC₅₀ value of 239 nM in human blood. ACT-672125 has activity for hERG with IC₅₀ value of 18μM. ACT-672125 can be used for the research of autoimmune diseases.