Tabimorelin hemifumarate

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2308/10
Tabimorelin hemifumarate | CAS No. 242143-80-2 | Ghrelin Receptor Agonists
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Description: Potent, orally active ghrelin receptor agonist
Alternative Names: NN 703

Chemical Name: N-[(2E)-5-Amino-5-methyl-1-oxo-2-hexenyl]-N-methyl-3-(2-naphthalenyl)-D-alanyl-N,Nα-dimethyl-D-phenylalaninamide hemifumarate

Purity: ≥98%

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Biological Activity

Tabimorelin hemifumarate is a potent, orally active ghrelin receptor (GHS-R1a) agonist (Ki = 50 nM at human recombinant GHS-R1a). Stimulates GH release from rat pituitary cells with an EC50 value of 2.7 nM. Induces hyperphagia and adiposity in lean rats, but not in leptin signaling-deficient ZDF rats.

Technical Data

M.Wt:
586.73
Formula:
C32H40N4O3.½C4H4O4
Solubility:
Soluble to 10 mM in water with gentle warming and to 100 mM in DMSO
Purity:
≥98%
Storage:
Desiccate at RT
CAS No:
242143-80-2

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. Pharmacological characterisation of a new oral GH secretagogue, NN703.
    Hansen et al.
    Eur.J.Endocrinol., 1999;141:180
  2. Adipogenic and orexigenic effects of the ghrelin-receptor ligand tabimorelin are diminished in leptin-signalling-deficient ZDF rats.
    Holm et al.
    Eur.J.Pharmacol., 2004;150:893

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