Calcium Flux Assay

HTS023RTA - Ready-to-Assay™ CRF1 Corticotropin Releasing Factor Receptor Frozen Cells

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    The CRF1 receptor is a Gs-coupled GPCR expressed in the brain and pituitary gland that binds to several neuropeptides, including corticotropin-releasing factor (CRF) and urocortin, and the amphibian peptide sauvagine (Chen et al., 1993;  Dautzenberg and Hauger, 2002;  Bale and Vale, 2004).  CRF plays a predominant role in stress response mediated by the hypothalamic-pituitary-adrenal axis, and alterations in CRF and its receptors CRF1 and CRF2 appear to be linked to depression and anxiety (Holsboer, 1999;  Bale and Vale, 2004).  A number of small molecule antagonists of the CRF1 receptor have been characterized, including R121919, SC241, NBI27914, antalarmin, DMP-696, and CP 154,526.  When delivered in animal models of psychiatric disorders, these antagonists display effectiveness in reducing stress-related behaviors (Kehne and De Lombaert, 2002). Cloned human CRF1-expressing cell line is made in the Chem-1 host, which supports high levels of recombinant CRF1 expression on the cell surface and contains high levels of the promiscuous G protein Gα15 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 CRF1.

    Additional Resource: HTS023RTA092614_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: X72304
    Protein Targets: Corticotropin
    Host Cell: Chem-1, an adherent rat hematopoietic cell line expressing endogenous Gα15 protein.
    Exogenous Gene Expression: CRF1 cDNA (Accession Number: X72304) expressed from a proprietary pHS plasmid.
    GMO: This product contains genetically modified organisms.
    Reference 1: 1. Bale TL and Vale WW (2004) CRF and CRF receptors: role in stress responsivity and other behaviors. Annu. Rev. Pharmacol. Toxicol. 44: 525-557.
    Reference 2: 2. Chen R., et al. (1993) Expression cloning of a human corticotropin-releasing factor receptor. Proc. Natl. Acad. Sci. USA 90: 8967-8971.
    Reference 3: 3. Dautzenberg FM and Hauger RL (2002) The CRF peptide family and their receptors: yet more partners discovered. Trends Pharmacol. Sci. 23: 71-77.
    Reference 4: 4. Holsboer F (1999) The rationale for cotricotropin-releasing hormone receptor (CRH-R) antagonists to treate depression and anxiety. J. Psychiatr. Res. 33: 181-214.
    Reference 5: 5. Kehne J and De Lombaert S (2002) Non-peptidic CRF1 receptor antagonists for the treatment of anxiety, depression and stress disorders. Curr Drug Targets CNS Neurol. Disord. 1: 467-493.