Calcium Flux Assay

HTS005RTA - Ready-to-Assay™ CCR1 Chemokine Receptor Frozen Cells

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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 agonists, antagonists and modulators at CCR1.

    Additional Resource: HTS005RTA092614_Datasheet

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    Item Unit of Measure: PK
    Contents: Pack contains 2 vials of mycoplasma-free cells, 1 ml per vial. Fifty (50) mL of Media Component.
    Storage: Vials are to be stored in liquid N2.
    Applications: Calcium Flux Assay
    Entrez Gene Number: L09230
    Protein Targets: CCR1
    Target Sub-family: Chemokine
    Species: Human
    Host Cell: Chem-1, an adherent rat hematopoietic cell line expressing endogenous Gα15 protein
    Exogenous Gene Expression: CCR1 cDNA (Accession Number: L09230) expressed from a proprietary plasmid.
    GMO: This product contains genetically modified organisms.
    Reference1: 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.