SML3222
TM-N1324
≥98% (HPLC)
Synonym(s):
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
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About This Item
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Quality Level
Assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
SMILES string
CC1=NN(C(N2)=C1C(C3=C(Cl)C=C(F)C=C3)CC2=O)C4=NC=NC5=C4NC=N5
General description
TM-N1324 also known as Cpd1324 is an agonist of GPR39, a G-protein-coupled receptor activated by Zn2+. GPR39 is a member of the ghrelin receptor family that has been implicated in the control of glucose-induced insulin secretion, pancreatic β-cell differentiation, control of lipolysis in white adipose tissue, and may also be involved in the pathophysiology of depression. TM-N1324 is found to activate human GPR39 with potencies of 280 nM and 9 nM in the absence and presence of Zn2+, respectively, and murine GPR39 with potencies of 180 nM and 5 nM in the absence and presence of Zn2+. TM-N1324 is known to stimulate gastric somatostatin secretion, indirectly inhibiting ghrelin secretion. It shows no agonist activity for 156 other GPCRs tested or for related receptors ghrelin and motilin. TM-N1324 serves as a tool to explore the physiological function of GPR39. It stimulates GLP-1 secretion in metabolic studies.
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
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Molecular metabolism, 49, 101207-101207 (2021-03-13)
Obesity is a complex disease associated with a high risk of comorbidities. Gastric bypass surgery, an invasive procedure with low patient eligibility, is currently the most effective intervention that achieves sustained weight loss. This beneficial effect is attributed to alterations
Journal of medicinal chemistry, 60(3), 886-898 (2017-01-04)
The G-protein-coupled receptor 39 (GPR39) is a G-protein-coupled receptor activated by Zn2+. We used a homology model-based approach to identify small-molecule pharmacological tool compounds for the receptor. The method focused on a putative binding site in GPR39 for synthetic ligands
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