Calcium Flux Assay

HTS005C - ChemiSCREEN™ Human Recombinant CCR1 Chemokine Receptor Calcium-Optimized Stable Cell Line

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    CCR1 is a GPCR that binds to a variety of CC ligands, including MIP-1a, RANTES, MCP-3, HCC-1, HCC-2, HCC-4, and MPIF-1 (Olson and Ley, 2002). Lymphocytes, macrophages, dendritic cells, and GM-CSF-activated neutrophils express CCR1 (Kaufmann et al., 2001; Cheng et al., 2001). Two selective, non-peptide small molecule antagonists of CCR1, BX-471 and CP-481,715, have been synthesized (Gladue et al., 2003; Liang et al., 2000). Pharmacological and genetic targeting of CCR1, either alone or in combination with cyclosporin A, reduces cardiac and renal allograft rejection (Gao et al., 2000; Horuk et al., 2001a; Horuk et al., 2001b), allergic encephalomyelitis (Liang et al., 2000), and renal fibrosis (Anders et al., 2002) in experimental models. Cloned human CCR1-expressing cell line is made in the Chem-1 host, which supports high levels of recombinant CCR1 expression on the cell surface and contains high levels of the promiscuous G protein Ga15 to couple the receptor to the calcium signaling pathway. Thus, the cell line is an ideal tool for screening for antagonists of interactions between CCR1 and its ligands.

    Additional Resource :  HTS005C082214 Datasheet

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    Storage: Vials are to be stored in liquid N2.
    Applications: Calcium Flux Assay, Ligand Binding Assay
    Host Cell: Chem-1, an adherent cell line expressing the promiscuous G-protein, Gα15.
    Exongenous Gene Expression: Human CCR1 cDNA (Accession Number: L09230)
    GMO: This product contains genetically modified organisms.
    Reference 1: 1. Anders, H.J., et al. (2002) A chemokine receptor CCR-1 antagonist reduces renal fibrosis after unilateral ureter ligation. J. Clin. Invest. 109: 251-9.
    Reference 2: 2. Cheng, S.S., et al. (2001) Granulocyte-macrophage colony stimulation factor up-regulates CCR1 in human neutrophils. J. Immunol. 166: 1178-84.
    Reference 3: 3. Gao, W., et al. (2000) Targeting of the chemokine recpetor CCR1 suppresses development of acute and chronic cardiac allograft rejection. J. Clin. Invest. 105: 35-44.
    Reference 4: 4. Gladue, R.P., et al. (2003) CP-481,715, a potent and selective CCR1 antagonist with potential therapeutic implications for inflammatory diseases. J. Biol. Chem. 278: 40473-80.
    Reference 5: 5. Horuk, R., et al. (2001a) CCR1-specific non-peptide antagonist: efficacy in a rabbit allograft rejection model. Immunol. Lett. 76: 193-201.
    Reference 6: 6. Horuk, R., et al. (2001b) A non-peptide functional antagonist of the CCR1 chemokine receptor is effective in rat heart transplant rejection. J. Biol. Chem. 276: 4199-4204.