A GPR39 agonist
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TM-N1324

Item No. 37208

Technical Information
Formal 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
CAS Number
1144477-35-9
Synonyms
  • Compound 1324
  • Cpd1324
Molecular Formula
C18H13ClFN7O
Formula Weight
Purity
≥98%
Formulation
A solid
DMSO: solubleEthanol: soluble
SMILES
O=C1NC2=C(C(C1)C3=CC=C(C=C3Cl)F)C(C)=NN2C4=NC=NC5=C4NC=N5
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)
InChi Key
CYQNVXRIWKKWQG-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    TM-N1324 is an agonist of G protein-coupled receptor 39 (GPR39).1 It is selective for GPR39 over a panel of 165 GPCRs, including the growth hormone (GH) secretagogue receptor (GHS-R) and motilin receptor, at 1 µM. TM-N1324 induces inositol phosphate accumulation in HEK293 cells expressing human GPR39 (EC50s = 2 and 201 nM in the presence and absence of zinc, respectively) and cAMP accumulation in COS-7 cells expressing human GPR39 (EC50 = 17 nM in the presence of zinc). It decreases ghrelin secretion and increases somatostatin secretion in isolated mouse gastric mucosa cells when used at a concentration of 1 µM. TM-N1324 (30 mg/kg) decreases food intake during the dark period and body weight in a mouse model of high-fat diet-induced obesity.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Frimurer, T.M., Mende, F., Graae, A.-S., et alModel-based discovery of synthetic agonists for the Zn2+-sensing G-protein-coupled receptor 39 (GPR39) reveals novel biological functions. J. Med. Chem. 60(3), 886-898 (2017).

    2. Grunddal, K.V., Diep, T.A., Petersen, N., et alSelective release of gastrointestinal hormones induced by an orally active GPR39 agonist. Mol. Metab. 49, 101207 (2021).