Catalog Number: 1946
Biological Activity
Broad spectrum neuropeptide antagonist/inverse agonist. Potent full inverse agonist for the ghrelin receptor (EC50 = 5.2 nM); diminishes constitutive ghrelin receptor signaling. Also antagonist at tachykinin, bradykinin, CCK and bombesin receptors. Induces apoptosis and inhibits cancer cell growth in vitro.
Technical Data
  • M.Wt:
    1516.85
  • Formula:
    C79H109N19O12
  • Sequence:
    RPKPFQWFWLL

    (Modifications: Arg-1 = D-Arg, Phe-5 = D-Phe, Trp-7 = Trp-9 = D-Trp, Leu-11 = C-terminal amide)

  • Solubility:
    Soluble to 1 mg/ml in water
  • Storage:
    Desiccate at -20°C
  • CAS No:
    96736-12-8
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. High constitutive signaling of the ghrelin receptor - identification of a potent inverse agonist.
    Holst et al.
    Mol.Endocrinol., 2003;17:2201
  2. [D-Arg1, D-Phe5, D-Trp7,9, Leu11] Substance P acts as a biased agonist toward neuropeptide and chemokine receptors.
    Jarpe et al.
    J.Biol.Chem., 1998;273:3097
  3. [D-Arg1, D-Phe5, D-Trp7,9, Leu11] Substance P induces apoptosis in lung cancer cells in vitro.
    Reeve and Bleehen
    Biochem.Biophys.Res.Commun., 1994;199:1313
Citations:

The citations listed below are publications that use Tocris products. Selected citations for [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P include:

3 Citations: Showing 1 - 3
Filter your results:

  1. A novel non-peptidic agonist of the ghrelin receptor with orexigenic activity In vivo
    Authors: Pastor-Cavada Et al.
    Scientific Reports 2016;6:36456
  2. Devil's Claw to suppress appetite--ghrelin receptor modulation potential of a Harpagophytum procumbens root extract.
    Authors: Torres-Fuentes Et al.
    Oncotarget 2014;9:e103118
  3. Promiscuous dimerization of the growth hormone secretagogue receptor (GHS-R1a) attenuates ghrelin-mediated signaling.
    Authors: Schellekens Et al.
    J Biol Chem 2013;288:181

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