Cyclosomatostatin

Cyclosomatostatin

Catalog Number:
L002372398APE
Mfr. No.:
APE-B7411
Price:
$459
  • Size:
    1mg
    Quantity:
    Add to Cart:
      • Overview
        • Please contact us at for specific academic pricing.

          Background

          IC50: N/A
          Cyclosomatostatin is a non-selective somatostatin receptor antagonist.
          Somatostatin is a regulatory hormone or tissue factor playing an inhibitory role in the normal regulation of several organ systems including hypothalamus and pituitary gland, central nervous system, gastrointestinal tract as well as pancreas.
          In vitro: Although cyclosomatostatin could fully block the effect of somatostatin, it only partially reversed the inhibitory effect of cortistatin, a new anti-inflammatory peptide. This observation was further supported by the fact that cyclosomatostatin reversed the antiinfl ammatory effect of somatostatin and octreotide in vitro completely, while only partially reversing the effect of cortistatin [1].
          In vivo: The effect of cortistatin was found to be dose dependent, with dose as low as 0.5 nmol (50 μg/kg) being partially protective. In contrast, cyclosomatostatin, somatostatin as well as octreotide were not protective [1].
          Clinical trial: As the precursor of cyclosomatostatin, somatostatin has already been introduced in the clinical practice in some macrophage populations. Somatostatin shows protective effect in certain inflammatory disorders including pancreatitis and liver injury. However, somatostatin is not protective in lethal septic shock [1].

      • Properties
        • Categories
          somatostatin receptor antagonist
          Alternative Name
          (3S,6R,9S,12S)-9-((1H-indol-3-yl)methyl)-6-(4-aminobutyl)-12-benzyl-3-((R)-1-(benzyloxy)ethyl)-1,4,7,10,13-pentaazacycloicosane-2,5,8,11,14-pentaone
          CAS Number
          84211-54-1
          Molecular Formula
          C44H57N7O6
          Molecular Weight
          779.98
          Appearance
          White lyophilised solid
          Purity
          98.00%
          Solubility
          Soluble to 1 mg/ml in 20% ethanol / H2O
          Storage
          Store at -20°C
          SMILES
          O=C([[email protected]@H](CCCCN)NC([[email protected]](CC1=CNC2=CC=CC=C12)NC([[email protected]](CC3=CC=CC=C3)NC4=O)=O)=O)N[[email protected]](C(NCCCCCC4)=O)[[email protected]@H](C)OCC5=CC=CC=C5

          * For Research Use Only

      • Reference
        • 1. Yue M, Xia et al. "Berberine ameliorates collagen-induced arthritis in rats by suppressing Th17 cell responses via inducing cortistatin in the gut." FEBS J. 2017 Sep;284(17):2786-2801. PMID:28636167

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