HTS139M - ChemiSCREEN™ sst5 Somatostatin Receptor Membrane Preparation

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    Somatostatin (sst) is a multifunctional peptide with two biologically active forms, sst-14 and sst-28, which are synthesized in neurons throughout the brain as well as in peripheral tissues such as the pancreas and the gut (Gillies, 1997). SST exerts a diverse array of effects that include inhibition of endocrine secretion, modulation of neurotransmission, and regulation of cell proliferation by stimulating a family of five G-protein-coupled receptors. Somatostatin receptor sst5 is an inhibitory G protein-coupled receptor that exerts a strong cytostatic effect on various cell types. In mice, sst5 mediates inhibition by somatostatin of pancreatic insulin secretion and contributes to the regulation of glucose homeostasis and insulin sensitivity (Strowski et al. 2003). In addition, deficiency of sst5 leads to subtype-selective sexually dimorphic changes in the expression of both brain and pancreatic somatostatins (Ramirez et al. 2004). sst5 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 agonists and antagonists of sst5. The membrane preparations exhibit a Kd of 1.2 nM for [125I]-Somatostatin 14. With 0.5 nM [125I]-Somatostatin 14, 5mg/well sst5 Membrane Prep typically yields greater than 10-fold signal-to-background ratio.

    Additional Resource :  HTS139M240914 Datasheet

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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
    Host Cell: Chem-1, an adherent mammalian cell line without any endogenous sst5 expression.
    Reference 1: 1.Gillies G (1997) Somatostatin: the neuroendocrine story. Trends Pharmacol. Sci. 18(3):87-95.
    Reference 2: 2. Strowski MZ et al. (2003). Somatostatin receptor subtype 5 regulates insulin secretion and glucose homeostasis. Mol. Endocrinol. 17: 93–106.
    Reference 3: 3. Ramirez, JL et al. (2004) Deficiency of somatostatin (SST) receptor type 5 (SSTR5) is associated with sexually dimorphic changes in the expression of SST and SST receptors in brain and pancreas. Mol. Cell. Endocrinol. 221: 105–119.