HTS005M - ChemiSCREEN™ CCR1 Chemokine Receptor Membrane Preparation

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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. CCR1 Membrane Preparations are ideal for screening molecules that disrupt interactions between CCR1 and its ligands. The CCR1 Membrane Preps bind to MIP-1a with a Kd of 1.8 nM, and yield greater than a 10-fold signal-to-background ratio with [125I]-MIP-1a at a concentration of 0.1 nM.

    Additional Resource :  HTS005M090314 Datasheet

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    Item Unit of Measure: EA
    Quantity: 200 units
    Storage: On receipt of material store at -70°C. Unopened reagent is stable for a minimum of 1 year from date of shipment when stored at recommended storage temperature. Avoid repeat freeze/thaw cycles.
    Applications: Radioligand Binding Assay
    Host Cell: Chem-2.
    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