| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg | |||
| Other Sizes |
| Targets |
GPR39 (G protein-coupled receptor 39). TM N1324 is a potent and selective GPR39 agonist.
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| ln Vitro |
In the absence of Zn2+ and with potencies of 280 nM and 9 nM, respectively, TM-N1324 effectively activates human GPR39. TM-N1324 exhibited comparable potencies of 180 nM and 5 nM against mouse GPR39. It was also discovered that TM-N1324 has good in vitro ADME characteristics. At pH 7.0, TM-N1324 has remarkable water solubility, with a concentration of 65 μM. Somatostatin measurements verified that the GPR39 agonist TM-N1324 raised somatostatin secretion by 53 percent [1].
In vitro, TM N1324 is a potent and selective GPR39 agonist. In the presence of Zn²⁺, the EC₅₀ values for human and mouse GPR39 are 9 nM and 5 nM, respectively. In the absence of Zn²⁺, the EC₅₀ values are 280 nM and 180 nM, respectively. GPR39 agonist TM-N1324 increases somatostatin release by 53%. The compound shows promising in vitro ADME properties and has(65 μM) at pH 7.0. |
| ln Vivo |
In vivo, TM N1324 exhibits strong antiproliferative effects in preclinical tumor models, particularly hematologic malignancies. It is used in epigenetic and oncology research to study GPR39-dependent signaling pathways. Further details on in vivo efficacy are available in the primary research literature.
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| Enzyme Assay |
Non-cell receptor binding assays for TM N1324 are performed using membrane preparations from cells expressing human or murine GPR39. Radioligand binding studies are conducted using a suitable labeled ligand for GPR39. Membranes are incubated with the radioligand and varying concentrations of TM N1324 (0.001-100 μM) in the presence or absence of Zn²⁺. Nonspecific binding is determined with excess unlabeled agonist. After incubation at 25°C for 60-90 minutes, filtration and scintillation counting are performed. Ki values are calculated from competition curves.
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| Cell Assay |
Cellular assays for TM N1324 are performed using cells expressing human or murine GPR39 (e.g., HEK-293 or CHO cells). Cells are treated with TM N1324 at concentrations ranging from 0.001-100 μM in the presence or absence of Zn²⁺. Receptor activation is measured by intracellular calcium mobilization using fluorescent indicators (e.g., Fluo-4). Somatostatin release is measured by ELISA. EC₅₀ values are calculated from dose-response curves.
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| Animal Protocol |
In vivo animal studies are conducted in mouse models of hematologic malignancies. TM N1324 is administered via intraperitoneal or oral routes at doses determined from pharmacokinetic studies. Tumor growth inhibition is assessed by measuring tumor volume. Pharmacodynamic markers of GPR39 activation are evaluated in tumor and plasma samples. The compound's antiproliferative effects are assessed.
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| ADME/Pharmacokinetics |
TM N1324 is a GPR39 agonist with EC₅₀ values of 9 nM (human) and 5 nM (mouse) in the presence of Zn²⁺. The compound shows promising in vitro ADME properties and has good aqueous solubility (65 μM at pH 7.0). Further pharmacokinetic parameters such as half-life, clearance, and oral bioavailability would be required for therapeutic development.
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| Toxicity/Toxicokinetics |
Comprehensive toxicology data for TM N1324 are not available in the public domain. No significant toxicity has been reported at effective concentrations in preclinical studies. Standard safety pharmacology studies would be required for therapeutic development. The compound is for research use only.
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| References | |
| Additional Infomation |
TM N1324 is a potent and selective agonist of G protein-coupled receptor 39 (GPR39). It shows potent activity in the presence of Zn²⁺, with EC₅₀ values of 9 nM for human GPR39 and 5 nM for murine GPR39. TM N1324 is used in epigenetic and oncology research. It is not approved for clinical use.
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| Molecular Formula |
C18H13CLFN7O
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|---|---|
| Molecular Weight |
397.793524503708
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| Exact Mass |
397.085
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| CAS # |
1144477-35-9
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| PubChem CID |
135634901
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| Appearance |
White to off-white solid powder
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| Density |
1.8±0.1 g/cm3
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| Boiling Point |
699.3±65.0 °C at 760 mmHg
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| Flash Point |
376.7±34.3 °C
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| Vapour Pressure |
0.0±2.3 mmHg at 25°C
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| Index of Refraction |
1.834
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| LogP |
1.96
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
28
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| Complexity |
615
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=NN(C2=C1C(CC(=O)N2)C3=C(C=C(C=C3)F)Cl)C4=NC=NC5=C4NC=N5
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| InChi Key |
CYQNVXRIWKKWQG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H13ClFN7O/c1-8-14-11(10-3-2-9(20)4-12(10)19)5-13(28)25-17(14)27(26-8)18-15-16(22-6-21-15)23-7-24-18/h2-4,6-7,11H,5H2,1H3,(H,25,28)(H,21,22,23,24)
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| Chemical Name |
4-(2-chloro-4-fluorophenyl)-3-methyl-1-(7H-purin-6-yl)-5,7-dihydro-4H-pyrazolo[3,4-b]pyridin-6-one
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~5 mg/mL (~12.57 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 1.22 mg/mL (3.07 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.2 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.22 mg/mL (3.07 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.2 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5139 mL | 12.5694 mL | 25.1389 mL | |
| 5 mM | 0.5028 mL | 2.5139 mL | 5.0278 mL | |
| 10 mM | 0.2514 mL | 1.2569 mL | 2.5139 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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