VU0453379 Chemical Properties

Boiling point:

671.8±55.0 °C(Predicted)

Density 

1.28±0.1 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

Soluble in DMSO

form 

Solid

pka

13.46±0.20(Predicted)

color 

Off-white to light yellow

Water Solubility 

H2O: 20mg/mL, clear

InChIKey

OCMGNMGYQPPMFF-FYZYNONXSA-N

SMILES

CN1C2=C(C(C(NC[C@@H]3CCCN3C(C)C)=O)=CN(C4CCCC4)C2=O)C5=CC=CC=C51.Cl

Safety Information

WGK Germany 

WGK 3

Storage Class

11 - Combustible Solids

VU0453379 Usage And Synthesis

Uses

VU0453379 is a highly selective and central nervous system (CNS) penetrant positive allosteric modulator (PAM) of glucagon-like peptide-1R (GLP-1R) with an EC50 of 1.3 μM[1].

Biological Activity

VU0453379 is a highly selective CNS penetrant positive allosteric modulator of Glucagon-like peptide-1 (GLP-1) with GLP-1 EC50 = 1.3 μ,M, 59.2% GLP-1 max. VU0453379 potentiated low-dose exenatide to augment insulin secretion in primary mouse pancreatic islets. In a model of Parkinson′s disease it showed a significant reversal of haloperidol-induced catalepsy at 30 mg/kg.

References

[1] Morris LC, et al. Discovery of (S)-2-cyclopentyl-N-((1-isopropylpyrrolidin2-yl)-9-methyl-1-oxo-2,9-dihydro-1H-pyrrido[3,4-b]indole-4-carboxamide (VU0453379): a novel, CNS penetrant glucagon-like peptide 1 receptor (GLP-1R) positive allosteric modulator (PAM). J Med Chem. 2014 Dec 11;57(23):10192-7. DOI:10.1021/jm501375c

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