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SML3222

Sigma-Aldrich

TM-N1324

≥98% (HPLC)

Sinônimo(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

Fórmula empírica (Notação de Hill):
C18H13ClFN7O
Número CAS:
1144477-35-9
Peso molecular:
397.79
Código UNSPSC:
12352107
NACRES:
NA.77

Nível de qualidade

100

Ensaio

≥98% (HPLC)

forma

powder

cor

white to beige

solubilidade

DMSO: 2 mg/mL, clear

temperatura de armazenamento

2-8°C

cadeia de caracteres SMILES

CC1=NN(C(N2)=C1C(C3=C(Cl)C=C(F)C=C3)CC2=O)C4=NC=NC5=C4NC=N5

Descrição geral

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.

Código de classe de armazenamento

11 - Combustible Solids

Classe de risco de água (WGK)

WGK 3

Ponto de fulgor (°F)

Not applicable

Ponto de fulgor (°C)

Not applicable

Certificados de análise (COA)

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Thomas M Frimurer et al.
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
Kaare V Grunddal et al.
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

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