HTS046M - ChemiSCREEN™ ETB Endothelin Receptor Membrane Preparation

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    The endothelin family of peptides is 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. Thus, the ETB Membrane Preparation is an ideal tool for screening for compounds binding to ETB. The membrane preparations exhibit a Kd of 0.03-0.06 nM for [125I]-endothelin-1. With 0.2 nM [125I]-endothelin-1, 10 mg/well ETB Membrane Prep yields greater than 5 fold signal-to-background ratio.

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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: Human ETB isoform 1 (Accession Number: NM_00015)
    Host Cell: CHO (Chinese hamster ovary cells)
    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.