2. GPCR/G Protein
    Immunology/Inflammation
  3. CCR

CCR

CCR (Chemokine receptors) are cytokine receptors found on the surface of certain cells that interact with a type of cytokine called achemokine. There have been 19 distinct chemokine receptors described in mammals. Each has a 7-transmembrane (7TM) structure and couples to G-protein for signal transduction within a cell, making them members of a large protein family of G protein-coupled receptors. Following interaction with their specific chemokine ligands, chemokine receptors trigger a flux in intracellular calcium (Ca2+) ions (calcium signaling). This causes cell responses, including the onset of a process known as chemotaxis that traffics the cell to a desired location within the organism. Chemokine receptors are divided into different families, CXC chemokine receptors, CC chemokine receptors, CX3C chemokine receptors and XC chemokine receptors that correspond to the 4 distinct subfamilies of chemokines they bind. Specific chemokine receptors provide the portals for HIV to get into cells, and others contribute to inflammatory diseases and cancer.

CCR Related Products (117):

Cat. No. Product Name Effect Purity
  • HY-15418
    RS 504393 Antagonist 99.43%
    RS 504393 is a selective CCR2 chemokine receptor antagonist (IC50 values are 89 nM and > 100 μM for inhibition of human recombinant CCR2 and CCR1 receptors respectively).
  • HY-B0673
    Pirfenidone Inhibitor 99.95%
    Pirfenidone (AMR69) is an antifibrotic agent that attenuates CCL2 and CCL12 production in fibrocyte cells. Pirfenidone has growth-inhibitory effect and reduces TGF-β2 protein levels in human glioma cell lines. Pirfenidone also has anti-inflammatory activities[1][2][3].
  • HY-50674
    INCB3344 Antagonist 99.73%
    INCB3344 is a potent, selective and orally bioavailable CCR2 antagonist with IC50 values of 5.1 nM (hCCR2) and 9.5 nM (mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM (mCCR2) in antagonism of chemotaxis activity.
  • HY-13004
    Maraviroc Antagonist 99.71%
    Maraviroc (UK-427857) is a selective CCR5 antagonist with activity against human HIV.
  • HY-B0498
    Bindarit Inhibitor 99.68%
    Bindarit (AF2838) is a selective inhibitor of the monocyte chemotactic proteins MCP-1/CCL2, MCP-3/CCL7, and MCP-2/CCL8, and no effect on other CC and CXC chemokines such as MIP-1α/CCL3, MIP-1β/CCL4, MIP-3/CCL23. Bindarit also has anti-inflammatory activity[1].
  • HY-103360B
    trans-J-113863 Antagonist
    trans-J-113863 is a potent chemokine CCR1 and CCR3 receptor antagonist, and inhibits MIP-1α-induced chemotaxis in CCR1 transfectants and eotaxin-induced chemotaxis in CCR3 transfectants with IC50 of 9.57 and 93.8 nM,respectively[1][2].
  • HY-160647
    CCR8 antagonist 3 Antagonist
    CCR8 antagonist 3 (compound 2) is a CCR8 antagonist with an IC50 value of 0.062 µM. CCR8 antagonist 3 shows human microsomal stability[1].
  • HY-160658
    AZ760 Antagonist
    AZ760 is a CCR8 antagonist. AZ760 shows excellent potency, good lipophilicity and high free fraction in blood. AZ760 exhibits unacceptable hERG inhibition[1].
  • HY-12080A
    BX471 hydrochloride Antagonist 99.94%
    BX471 hydrochloride (ZK-811752 hydrochloride) is a potent, selective non-peptide CCR1 antagonist with Ki of 1 nM for human CCR1, and exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4.
  • HY-114097A
    CCR1 antagonist 11 hydrochloride Antagonist
    CCR1 antagonist 11 hydrochloride (A1B1) is an orally active CCR1 antagonist with the IC50 values of 0.03 μM, 0.58 μM and 0.32 μM for hCCR1, mCCR1 and rCCR1, respectively. CCR1 antagonist 11 hydrochloride can be used in the study of rheumatoid arthritis and other related inflammatory diseases[1].
  • HY-111069
    Nifeviroc Inhibitor 98.17%
    Nifeviroc is an orally active CCR5 antagonist. Nifeviroc is used for the study of HIV type-1 infection[1].
  • HY-152132
    CCR5 antagonist 3 Inhibitor
    CCR5 antagonist 3 (Compound 26) is a CCR5 antagonist with an IC50 of 15.90 nM. CCR5 antagonist 3 shows broad-spectrum anti-HIV-1 activities[1].
  • HY-15544
    CCR1 antagonist 10 Antagonist
    CCR1 antagonist 10 (example 1) is a potent and orally active CCR1 antagonist. CCR1 antagonist 10 inhibits 125I-MIP-1α binding to THP-1 cell membranes with an Ki value of 2.3 nM[1].
  • HY-107051
    GW 766994 Antagonist 98.77%
    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[1][2].
  • HY-119101
    AZD-5672 Antagonist
    AZD-5672 is an orally active, potent, and selective CCR5 antagonist (IC50=0.32 nM). AZD-5672 shows moderate activity against the hERG ion channel (binding IC50=7.3 μM). AZD5672 is a substrate of human P-gp, and inhibits P-gp-mediated digoxin transport (IC50=32 μM). AZD-5672 can be used for the research of rheumatoid arthritis[1][2][3].
  • HY-50669A
    MK-0812 Succinate Antagonist 99.94%
    MK-0812 Succinate is a potent and selective CCR2 antagonist with high affinity at CCR2.
  • HY-136788
    ALK4290 Inhibitor 99.21%
    ALK4290 (AKST4290) is a potent and orally active CCR3 inhibitor extracted from patent US20130261153A1, compound Example 2, with a Ki of 3.2 nM for hCCR3[1]. ALK4290 can be used for the research of neovascular age-related macular degeneration and Parkinsonism[2][3].
  • HY-N2609
    7,4'-Dihydroxyflavone Inhibitor 99.68%
    7,4'-Dihydroxyflavone (7,4'-DHF) is a flavonoid, which can be isolated from Glycyrrhiza uralensis. 7,4'-Dihydroxyflavone is eotaxin/CCL11 inhibitor and CBR1 inhibitor (IC50=0.28 μM). 7,4'-Dihydroxyflavone has the ability to consistently suppress eotaxin production and prevent dexamethasone (Dex)‐paradoxical adverse effects on eotaxin production[1]. 7,4'-Dihydroxyflavone (7,4'-DHF) inhibits MUC5AC gene expression, mucus production and secretion via regulation of NF-κB, STAT6 and HDAC2.7,4'-Dihydroxyflavone (7,4'-DHF) decreases phorbol 12-myristate 13-acetate (PMA) stimulated NCI-H292 human airway epithelial cell MUC5AC gene expression and mucus production with IC50 value of 1.4 µM[1].
  • HY-14231
    CCR5 antagonist 5 Antagonist
    CCR5 antagonist 5 (compound example 11) is a CCR5 antagonist. CCR5 antagonist 5 has the potential to study inflammation and immunity and viral (such as HIV) infection[1].
  • HY-111321
    Fuscin Inhibitor
    Fuscin, a fungal metabolite, CCR5 receptor antagonist with anti-HIV effects. Fuscin is a respiration and oxidative phosphorylation inhibitor, and also a mitochondrial SH-dependent transport-linked functions inhibitor[1][2][3].