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Submit ReviewTabimorelin hemifumarate
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% (HPLC)
Biological Activity for Tabimorelin hemifumarate
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 for Tabimorelin hemifumarate
| M. Wt | 586.73 |
| Formula | C32H40N4O3.½C4H4O4 |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 242143-80-2 |
| PubChem ID | 11981159 |
| InChI Key | YQDJPWXYLLPOPW-LWTUVRFUSA-N |
| Smiles | [H]OC(=O)\C=C\C(=O)O[H].CNC(=O)[C@@H](CC1=CC=CC=C1)N(C)C(=O)[C@@H](CC1=CC2=CC=CC=C2C=C1)N(C)C(=O)\C=C\CC(C)(C)N.CNC(=O)[C@@H](CC1=CC=CC=C1)N(C)C(=O)[C@@H](CC1=CC2=CC=CC=C2C=C1)N(C)C(=O)\C=C\CC(C)(C)N |
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.
Solubility Data for Tabimorelin hemifumarate
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 5.29 | 10 with gentle warming | |
| DMSO | 58.67 | 100 |
Preparing Stock Solutions for Tabimorelin hemifumarate
The following data is based on the product molecular weight 586.73. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.7 mL | 8.52 mL | 17.04 mL |
| 5 mM | 0.34 mL | 1.7 mL | 3.41 mL |
| 10 mM | 0.17 mL | 0.85 mL | 1.7 mL |
| 50 mM | 0.03 mL | 0.17 mL | 0.34 mL |
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Product Datasheets for Tabimorelin hemifumarate
References for Tabimorelin hemifumarate
References are publications that support the biological activity of the product.
Hansen et al (1999) Pharmacological characterisation of a new oral GH secretagogue, NN703. Eur.J.Endocrinol. 141 180 PMID: 10427162
Holm et al (2004) Adipogenic and orexigenic effects of the ghrelin-receptor ligand tabimorelin are diminished in leptin-signalling-deficient ZDF rats. Eur.J.Pharmacol. 150 893 PMID: 15191361
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Keywords: Tabimorelin hemifumarate, Tabimorelin hemifumarate supplier, Potent, orally, active, ghrelin, receptor, agonists, GHS-R1a, Receptors, Growth, Hormone, Secretagog, 1a, NN703, NN, 703, Ghrelin, 2308, Tocris Bioscience
Citations for Tabimorelin hemifumarate
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Literature in this Area
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Peptides Involved in Appetite Modulation Scientific Review
Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.