Calcium Flux Assay

HTS024RTA - Ready-to-Assay™ CRF2 Corticotropin Releasing Factor Receptor Frozen Cells

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HTS024RTA
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    The corticotropin-releasing factor receptors, CRF1 and CRF2, are Gs-coupled GPCRs expressed in the brain, blood vessels and intestine that bind to several neuropeptides, including corticotropin-releasing factor (CRF) and urocortin, and the amphibian peptide sauvagine (Lovenberg et al., 1995;  Bale and Vale, 2004).  In addition, two peptides, urocortin II (Ucn II) and urocortin III (Ucn III), bind selectively and with high affinity to CRF2 (Lewis et al., 2001).  The CRF peptides and their receptors play important roles in stress mediated by the hypothalamic-pituitary-adrenal axis in animal models, and possibly in depression and anxiety in humans, although the contributions of CRF1 and CRF2 appear to be distinct (Bale and Vale, 2004;  Risbrough et al., 2004)  In addition, CRF1 and CRF2 differentially alter feeding behavior, gastric motility and vascular tone (Zorrilla et al., 2004;  Martinez et al., 2004;  Wiley and Davenport, 2004).  Cloned human CRF2-expressing cell line is made in the Chem-1 host, which supports high levels of recombinant CRF2 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 CRF2.

    Additional Resource: HTS024RTA092614_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: NM_001883
    Protein Targets: CRF2
    Target Sub-family: Corticotropin
    Host Cell: Chem-1, an adherent rat hematopoietic cell line expressing endogenous Gα15 protein.
    Exogenous Gene Expression: CRF2 cDNA (Accession Number: NM_001883; see CODING SEQUENCE below) expressed from a proprietary 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. Lewis K et al. (2001) Identification of urocortin III, an additional member of the corticotropin-releasing factor (CRF) family with high affinity for the CRF2 receptor. Proc. Natl. Acad. Sci. USA 98: 7570-7575.
    Reference 3: 3. Lovenberg TW et al. (1995) Cloning and characterization of a functionally distinct corticoptropin-releasing factor receptor subtype from rat brain. Proc. Natl. Acad. Sci. USA 92: 836-840.
    Reference 4: 4. Martinez V et al. (2004) Central CRF, urocortins and stress increase colonic transit via CRF1 receptors while activation of CRF2 receptors delays gastric transit in mice. J. Physiol. 556: 221-234.
    Reference 5: 5. Risbrough VB et al. (2004) Corticotropin-releasing factor receptors CRF1 and CRF2 exert both additive and opposing influences on defensive startle behavior. J. Neurosci. 24: 6545-6552.
    Reference 6: 6. Wiley KE and Davenport AP (2004) CRF2 receptors are highly expressed in the human cardiovascular system and their cognate ligands urocortins 2 and 3 are potent vasodilators. Br. J. Pharmacol. 143: 508-514.
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