1144477-35-9
1144477-35-9 structure
- Name: TM N1324
- Chemical Name: TM-N1324
- CAS Number: 1144477-35-9
- Molecular Formula: C18H13ClFN7O
- Molecular Weight: 397.793
- Catalog: Signaling Pathways GPCR/G Protein GHSR
- Create Date: 2018-06-28 06:35:29
- Modify Date: 2024-01-17 19:11:01
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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.
| Name | TM-N1324 |
|---|---|
| Synonyms |
1H-Pyrazolo[3,4-b]pyridin-6-ol, 4-(2-chloro-4-fluorophenyl)-4,5-dihydro-3-methyl-1-(9H-purin-6-yl)-
4-(2-Chloro-4-fluorophenyl)-3-methyl-1-(1H-purin-6-yl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-b]pyridin-6-one |
| Description | 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. |
|---|---|
| Related Catalog | |
| Target |
EC50: 280 nM (human GPR39 without Zn2+), 9 nM (human GPR39 with Zn2+), 180 nM (murine GPR39 without Zn2+), 5 nM (murine GPR39 with Zn2+)[1] |
| In Vitro | 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]. |
| Cell Assay | Caco-2 cells are used as an in vitro model of the human intestinal epithelium and permit assessment of the intestinal permeability of TM-N1324. TM-N1324 is added to either the apical or basolateral side of a confluent monolayer of Caco-2 cells and permeability is measured by monitoring the appearance of the TM-N1324 on the opposite side of the membrane using LC-MS/MS. TM-N1324 (3 µM) is incubated with pooled liver microsomes and incubated at 5 time points over the course of a 45 min experiment finally TM-N1324 is analyzed by LC-MS/MS. The intrinsic clearance (CLint) and t1/2 values for TM-N1324 in human and mouse microsomes are reported[1]. |
| References |
| Density | 1.8±0.1 g/cm3 |
|---|---|
| Boiling Point | 699.3±65.0 °C at 760 mmHg |
| Molecular Formula | C18H13ClFN7O |
| Molecular Weight | 397.793 |
| Flash Point | 376.7±34.3 °C |
| Exact Mass | 397.085419 |
| LogP | 1.96 |
| Vapour Pressure | 0.0±2.3 mmHg at 25°C |
| Index of Refraction | 1.834 |
| Storage condition | 2-8℃ |