TM-N1324 (Synonyms: Compound 1324, Cpd1324) |
| Katalog-Nr.GC31074 |
TM-N1324 ist ein Agonist des G-Protein-gekoppelten Rezeptors 39 (GPR39) mit EC50-Werten von 9 nM/5 nM in Gegenwart von Zn2+ und 280 nM/180 nM in Abwesenheit von Zn2+ fÜr menschliches/murines GPR39.
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Cas No.: 1144477-35-9
Sample solution is provided at 25 µL, 10mM.
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TM-N1324 is an agonist of G-Protein-Coupled Receptor 39 (GPR39) with EC50s of 9 nM/5 nM in the presence of Zn2+, and 280 nM/180 nM in the absence of Zn2+ for human/murine GPR39.
TM-N1324 activates human GPR39 with high efficacy and potencies of 280 nM and 9 nM in the absence and presence of Zn2+, respectively. TM-N1324 has similar potencies on murine GPR39, 180 nM and 5 nM. TM-N1324 is also found to have promising in vitro ADME properties. TM-N1324 has reasonably good aqueous solubility (65 μM at pH 7.0). Measurements of somatostatin confirms that the GPR39 agonist TM-N1324 increases somatostatin release by 53%[1].
[1]. Frimurer TM, et al. Model-Based Discovery of Synthetic Agonists for the Zn2+-Sensing G-Protein-Coupled Receptor 39 (GPR39) Reveals Novel Biological Functions. J Med Chem. 2017 Feb 9;60(3):886-898.
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