CCR3 Antagonist

SB-328437 is a potent, selective non-peptide CCR3 antagonist with an IC₅₀ of 4.5 nM. SB-328437 can inhibit eosinophil migration induced by eotaxin, eotaxin-2, and monocyte chemotactic protein-4. In addition, SB-328437 can sensitize 5-FU (HY-90006)-resistant gastric cancer cells. SB-328437 can also reduce the recruitment of neutrophils to the lungs and pulmonary inflammation during acute inflammation. SB-328437 can be used in the research of inflammation-related diseases.

J-113863 is a potent and selective CCR1 antagonist with IC₅₀ values of 0.9 nM and 5.8 nM for human and mouse CCR1 receptors, respectively. J-113863 is also a potent antagonist of the human CCR3 (IC₅₀ of 0.58 nM) , but a weak antagonist of the mouse CCR3 (IC₅₀ of 460 nM). J-113863 is inactive against CCR2, CCR4 and CCR5, as well as the LTB4 or TNF-α receptors. Anti-inflammatory effect.

GW 766994 (GW 994) is an orally active and specific chemokine receptor-3 (CCR3) antagonist. GW 766994 has the potential for asthma and eosinophilic bronchitis research.

SB297006 is a CCR3 antagonist, which significantly inhibits proliferation and neurosphere formation in CCL11-treated neural progenitor cells.

YM-344484 is an orally active dual antagonist of chemokine CCR3 receptor and histamine histamine H1 receptor. YM-344484 inhibits ligand-induced Ca²⁺ influx, chemotaxis of CCR3-expressing cells, histamine-induced Ca²⁺ influx, increased vascular permeability and eosinophil accumulation. YM-344484 suppresses vascular permeability and inhibits eosinophil infiltration in a mouse asthma model. YM-344484 can be used in research related to asthma, allergic rhinitis and atopic dermatitis.

BMS-570520 is an orally bioavailable CCR3 antagonist with an IC₅₀ of 1.9 nM against hCCR3 and an IC₅₀ of 1300 nM against hCYP2D6. BMS-570520 inhibits CYP2D6, but shows low activity against off-target G protein-coupled receptors, biogenic amine transporters, and the hERG potassium channel. BMS-570520 regulates chemotaxis, calcium mobilization, and anti-inflammatory pathways. BMS-570520 can be used in research related to asthma, allergic rhinitis, and contact dermatitis.

CCR3 antagonist 1 is a potent antagonist of CCR3, used for the research of immunologic and inflammatory diseases.

YM-344031 is an orally active antagonist for CCR3. YM-344031 inhibits binding of Eotaxin-1 and RANTES to CCR3, with IC₅₀ of 3.0 and 16.3 nM. YM-344031 inhibits ligand-induced rise in intracellular Ca^[2+] and the ligand-induced chemotaxis. YM-344031 inhibits eotaxin-1-induced changes in eosinophil morphology in macaques blood, and prevents allergic skin reactions in a mouse allergy model.

Maceneolignan H (Compound 8) is a neolignane compound isolated from the arils of Myristica fragrans. Maceneolignan H is a selective CCR3 antagonist (EC₅₀ = 1.4 μM). Maceneolignan H has the potential for the research of allergic diseases.

BMS-639623 is a potent and orally activeCCR3 antagonist with an IC₅₀ of 0.3 nM. BMS-639623 picomolar inhibition potency against eosinophil chemotaxis (IC₅₀=38 pM). BMS-639623 can be used for the research of asthma.