L-803,087 trifluoroacetate

Catalog #: 1979 Datasheet / COA / SDS

Discontinued Product

1979 has been discontinued.
View all Somatostatin Receptor Agonists products.
L-803,087 trifluoroacetate | CAS No. 1786412-46-1 | Somatostatin Receptor Agonists
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Description: Potent and selective sst4 agonist

Chemical Name: N2-[4-(5,7-Difluoro-2-phenyl-1H-indol-3-yl)-1-oxobutyl]-L-arginine methyl ester trifluoroacetate

Purity: ≥97%

Product Details
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Biological Activity

L-803,087 trifluoroacetate is a potent and selective somatostatin sst4 receptor agonist. Ki values are 0.7, 199, 4720, 1280 and 3880 nM for cloned human sst4, sst1, sst2, sst3 and sst5 receptors respectively. Facilitates AMPA-mediated hippocampal synaptic responses in vitro and increases kainate-induced seizures in mice in vivo.

Technical Data

M.Wt:
599.56
Formula:
C25H29F2N5O3.CF3CO2H
Solubility:
Soluble to 100 mM in DMSO and to 100 mM in ethanol
Purity:
≥97%
Storage:
Store at -20°C
CAS No:
1786412-46-1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. Regulation of somatostatin receptor 4-mediated cytostatic effects by CD26 in malignant pleural mesothelioma.
    Yamamoto, J, Ohnuma, K, Hatano, R, Okamoto, T, Komiya, E, Yamazaki, H, Iwata, S, Dang, N H, Aoe, K, Kishimoto, T, Yamada, T, Morimoto, C
    Br J Cancer, 2014;110(9):2232-45.
  2. Identification and characterization of subtype selective somatostatin receptor agonists.
    Rohrer and Schaeffer
    J.Physiol.Paris, 2000;94:211
  3. Rapid identification of subtype-selective agonists of the somatostatin receptor through combinatorial chemistry.
    Rohrer et al.
    Science, 1998;282:737
  4. Somatostatin receptor subtypes 2 and 4 affect seizure susceptibility and hippocampal excitatory neurotransmission in mice.
    Moneta et al.
    Eur.J.Neurosci., 2002;16:843

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