ChemiSCREEN CCR1 Membrane Preparation

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. Chemicon′s CCR1 Membrane Preparations are ideal for screening molecules that disrupt interaction between CCR1 and its ligands. The CCR1 Membrane Preps bind to MIP-1a with a Kd of 1.8 nM, and yield greater than 10-fold signal to background ratio with a MIP-1a concentration of 0.1 nM.

Full-length human CCR1 cDNA

Radioligand binding assay.

GPCR Class: A

Protein Target: CCR1

Target Sub-Family: Chemokine

SPECIFICATIONS:
Bmax for [¹²⁵I]MIP-1alpha binding: 3.3 pmol/mg protein
K_d for [¹²⁵I] MIP-1alpha binding: ~ 1.8 nM HOST CELLS:

Liquid in packaging buffer: 50 mM Tris pH 7.4, 10% glycerol and 1% BSA with no preservatives.
Packaging method: Membranes protein were adjusted to the indicated concentration in packaging buffer, rapidly frozen, and stored at -80°C.
Each vial typically contains 500 units, where one unit is the amount of membrane prep that yields greater than 1000 cpm specific binding of ¹²⁵I-labeled MIP-1α (0.1 nM input concentration).

Maintain frozen at -70°C for up to 2 years. Do not freeze and thaw.

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