HTS046RTA - Ready-to-Assay™ ETB Endothelin Receptor Frozen Cells

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    The endothelin family of peptides are potent vasoconstrictors synthesized by endothelial cells in both constitutive and inducible pathways.  The biological actions of endothelins are mediated by two GPCRs, ETA and ETB (Davenport, 2002).   Whereas ETA is the predominant receptor on smooth muscle cells and thus is the primary mediator of the vasoconstrictor activity, ETB is found on endothelial cells and mediates vasodilation (Nilsson et al., 1997).  In addition, ETB has also been linked to renal failure, congestive heart failure, atherosclerosis, and pulmonary hypertension (D’Orléans-Juste, et al., 2002).  A mutation in ETB has been found to cause Hirschsprung disease-2, a degenerative disease of the digestive tract (Puffenberger et al, 1994). Cloned human ETB-expressing cell line is made in the CHO host, which supports high levels of recombinant ETB expression on the cell surface for functional detection via the calcium signaling pathway. Thus, the cell line is an ideal tool for screening for agonists, antagonists, and modulators at ETB.

    Additional Resource :  HTS046RTA092714 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. Media Component at 4ºC (-20ºC for prolonged storage).
    Applications: Calcium Flux Assay
    Host Cell: Chinese Hamster Ovarian K-1 cells (CHO K-1).
    Exongenous Gene Expression: EDNRB cDNA (Accession Number: NM_000115- see CODING SEQUENCE below) expressed from a proprietary pHS plasmid.
    GMO: This product contains genetically modified organisms.
    Reference 1: 1. Davenport AP (2002) International Union of Pharmacology. XXIX. Update on Endothelin Receptor Nomenclature. Pharmacol. Rev. 54: 219-226.
    Reference 2: 2. Nilsson T, et al. (1997) Presence of contractile endothelin-A and dilatory endothelin-B receptors in human cerebral arteries. Neurosurgery. 40: 346–351-comment 351–353.
    Reference 3: 3. D’Orléans-Juste P, et al (2002) Function of the endothelinB receptor in cardiovascular physiology and pathophysiology. Pharmacol Ther. 95: 221-238.
    Reference 4: 4. Puffenberger EG, et al (1994) A missense mutation of the endothelin-B receptor gene in multigenic Hirschsprung's disease. Cell 79: 1257-1266.