TargetMol

GLP-1R Agonist DMB

Product Code:
 
TAR-T36579
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20℃
1 / 1

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TAR-T36579-50mg50mgEnquire
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TAR-T36579-25mg25mg£412.00
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Further Information

Bioactivity:
GLP-1R agonist DMB is an agonist of glucagon-like peptide 1 receptor (GLP-1R; KB = 26.3 nM for the recombinant human receptor).1 It inhibits forskolin-induced cAMP accumulation in BHK cells expressing the recombinant human receptor with an EC50 value of 101 nM.2 GLP-1R (100 and 1,000 nM) increases insulin levels induced by D-(+)-glucose in pancreatic islets isolated from wild-type, but not Glp1r knockout, mice. It reduces fasting plasma glucose levels in mice when administered at a dose of 5 μmol/kg.3
CAS:
281209-71-0
Formula:
C13H15Cl2N3O2S
Molecular Weight:
348.24
Pathway:
GPCR/G Protein
Purity:
0.98
SMILES:
CC(C)(C)Nc1nc2cc(Cl)c(Cl)cc2nc1S(C)(=O)=O
Target:
Glucagon Receptor

References

Knudsen, L.B., Kiel, D., Teng, M., et al. Small-molecule agonists for the glucagon-like peptide 1 receptor. Proc. Natl. Acad. Sci. USA 104(3), 937-942 (2007). Irwin, N., Flatt, P.R., Patterson, S., et al. Insulin-releasing and metabolic effects of small molecule GLP-1 receptor agonist 6,7-dichloro-2-methylsulfonyl-3-N-tert-butylaminoquinoxaline. Eur. J. Pharmacol. 628(1-3), 268-273 (2010). Koole, C., Wootten, D., Simms, J., et al. Allosteric ligands of the glucagon-like peptide 1 receptor (GLP-1R) differentially modulate endogenous and exogenous peptide responses in a pathway-selective manner: Implications for drug screening. Mol. Pharmacol. 78(3), 456-465 (2010).