HTS022M - ChemiSCREEN™ MC3 Melanocortin Receptor Membrane Preparation

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    The melanocortins, the peptides a-, b- and g-melanocyte-stimulating hormone (MSH), bind to a family of five Gs-coupled GPCR receptors (MC1-5) and play important roles in energy balance, reproductive function, pigmentation and inflammation (Gantz and Fong, 2003). MC3 is expressed in the CNS, including the hypothalamus, and appears to play a role in energy homeostasis as indicated by the observation that MC3-null mice have increased subcutaneous fat, a loss of lean body mass, and reduced energy expenditure (Butler et al., 2000; Chen et al., 2000). Macrophages also express MC3, which together with MC1 mediates the anti-inflammatory activity of melanocortins in animal models of peritonitis and myocardial infarct (Getting et al., 2003; 2004). The MC3 membrane preparations are crude membrane preparations made from our proprietary stable recombinant cell lines to ensure high-level of GPCR surface expression; thus, they are ideal HTS tools for screening of antagonists of MC3 interactions with melanocortins. The membrane preparations exhibit a Kd of 0.4 nM for [125I]-MSH. With 10.0 mg/well MC3 Membrane Prep and 0.25 nM [125I]-MSH analog, a greater than 4-fold signal-to-background ratio is obtained.

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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. For maximum recovery of product, centrifuge original vial
    Applications: Radioligand Binding Assay
    Species: Full-length human MC3R cDNA encoding MC3 (Accession number L06155).
    Host Cell: Chem-1, an adherent mammalian cell line without any endogenous MC3 expression.
    Reference 1: 1. Butler AA et al. (2000) A unique metabolic syndrome causes obesity in the melanocortin-3 receptor-deficient mouse. Endocrinology 141: 3518-21.
    Reference 2: 2. Chen AS et al. (2000) Inactivation of the mouse melanocortin-3 receptor results in increased fat mass and reduced lean body mass. Nat. Genet. 26: 97-102.
    Reference 3: 3. Gantz I and Fong TM (2003) The melanocortin system. Am. J. Physiol. Endocrinol. Metab. 284: E468-E474.
    Reference 4: 4. Getting SJ et al. (2003) Redundancy of a functional melanocortin 1 receptor in the anti-inflammatory actions of melanocortin peptides: studies in the recessive yellow (e/e) mouse suggest an important role for melanocortin 3 receptor. J. Immunol.
    Reference 5: 5. Getting SJ et al. (2004) MC-3 receptor and the inflammatory mechanisms activated in acute myocardial infarct. J. Leukoc. Biol. 76: 845-53.