TM N1324

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Cat.No. 6325 - TM N1324 | C18H13ClFN7O | CAS No. 1144477-35-9
Description: Potent and selective GPR39 agonist; orally bioavailable
Chemical Name: 4-(2-Chloro-4-fluorophenyl)-1,4,5,7-tetrahydro-3-methyl-1-(9H-purin-6-yl)-6H-pyrazolo[3,4-b]pyridin-6-one
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

Potent and selective GPR39 agonist (IC50 values are 280 and 9 nM in the absence and presence of Zn2+, respectively). Exhibits no significant activity against a panel of 165 other GPCRs. Inhibits the release of ghrelin and somatostatin from primary gastric mucosa cells in vitro. Cell permeable and orally bioavailable.

Technical Data

M. Wt 397.79
Formula C18H13ClFN7O
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1144477-35-9
PubChem ID 42654322
InChI Key AAKZKVKEKKTMRJ-UHFFFAOYSA-N
Smiles CC1=NN(C2=C3NC=NC3=NC=N2)C4=C1C(C5=C(C=C(C=C5)F)Cl)CC(N4)=O

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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 3.98 10 with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 397.79. 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
0.1 mM 25.14 mL 125.69 mL 251.39 mL
0.5 mM 5.03 mL 25.14 mL 50.28 mL
1 mM 2.51 mL 12.57 mL 25.14 mL
5 mM 0.5 mL 2.51 mL 5.03 mL

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References

References are publications that support the biological activity of the product.

Frimurer et al (2017) Model-based discovery of synthetic agonists for the Zn2+-sensing G-protein-coupled receptor 39 (GPR39) reveals novel biological functions. J.Med.Chem. 60 886 PMID: 28045522


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Keywords: TM N1324, TM N1324 supplier, TMN1324, gpr39, agonists, agonism, potent, selective, orally, bioavailable, cell, permeable, zn2+, zinc, Orphan, 7-TM, Receptors, 6325, Tocris Bioscience

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Literature in this Area

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