ccr3

CCR3 antagonist 1 is a potent CCR3 antagonist used in researching inflammatory and immunologic diseases.

Trans-J-113863 serves as a potent antagonist of chemokine receptors CCR1 and CCR3, effectively inhibiting MIP-1α-induced chemotaxis in CCR1 transfectants and eotaxin-induced chemotaxis in CCR3 transfectants, with respective half-maximal inhibitory concentrations (IC50) of 9.57 nM and 93.8 nM [1] [2].

BMS-639623 is a CCR3 antagonist with a picomolar inhibitory effect on eosinophilic chemotaxis and can be used in the treatment of asthma.

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. J-113863 is a potent and selective CCR1 (CD18) antagonist with IC50 values of 0.9 nM and 5.8 nM for human and mouse CCR1 receptors, respectively.

chemokine CCR1 and CCR3 receptor antagonist

SB 328437 ((S)-methyl 2-(1-naphthamido)-3-(4-nitrophenyl)propanoate) is an effective and selective antagonist of CCR3 (IC50 = 4.5 nM).

GW 766994 is a specific and oral chemokine receptor-3 (CCR3) antagonist. It has the potential for asthma and eosinophilic bronchitis treatment.

ALK4290 dihydrochloride (AKST4290 dihydrochlorid) serves as a potent and orally active inhibitor of CCR3, exhibiting a K i of 3.2 nM for hCCR3 [1]. It is primarily used in research related to neovascular age-related macular degeneration and Parkinsonism [2] [3].

CKLF1-C19, the C-terminal peptide of human chemokine-like factor 1 (CKLF1), interacts with CCR4 and inhibits chemotaxis induced by CKLF1 and CCL17. It also suppresses allergic lung inflammation by inhibiting chemotaxis mediated by CCR3 and CCR4 [1].

Maceneolignan H (Compound 8), a neolignane derived from the arils of Myristica fragrans, acts as a selective CCR3 antagonist with an EC 50 value of 1.4 μM. This compound shows promise for allergic disease research [1].

CH-0076989 is a chemokine receptor CCR3 agonist.

ALK4290 (AKST4290) is a potent, orally active CCR3 inhibitor (compound Example 2) with a Ki of 3.2 nM for hCCR3[1], suitable for research into neovascular age-related macular degeneration and Parkinsonism[2][3].

SB297006 is an antagonist of C-C chemokine receptor 3 (CCR3; IC50 = 39 nM), which normally is activated by eotaxin, eotaxin-3, MCP-3, MCP-4, RANTES, and MIP-1δ. It is at least 250-fold selective for CCR3 over a panel of other chemokine receptors. SB 297006 blocks CCR3-mediated calcium mobilization induced by eotaxin, eotaxin-2, and MCP-4 in transfected cells. It suppresses antigen-induced accumulation of Th2 lymphocytes and eosinophils in lungs of mice when delivered subcutaneously (100 mg kg).