1638646-27-1
Chemical Structure
VU0453379
- CAS No.: 1638646-27-1
- Formula:C26H34N4O2
- Molecular Weight:434.57
IUPAC Name: (S)-2-cyclopentyl-N-((1-isopropylpyrrolidin-2-yl)methyl)-9-methyl-1-oxo-2,9-dihydro-1H-pyrido[3,4-b]indole-4-carboxamide
InChIKey: OEYYOVRNPJSWTO-IBGZPJMESA-N
SMILES: O=C(NC[C@H]1N(CCC1)C(C)C)C(C2=C3N(C4=C2C=CC=C4)C)=CN(C3=O)C5CCCC5
Biological Activity: VU0453379 is a blood-brain barrier permeable GLP-1R positive allosteric modulator (PAM) with an EC50 value of 1.3 μM. VU0453379 potentiates the actions of endogenous GLP-1 and synthetic peptide agonists, and promotes GLP-1 receptor internalization. VU0453379 stimulates insulin secretion from primary mouse islets. VU0453379 enhances the function of endogenous GLP-1R and reverses catalepsy in animal models. VU0453379 is useful for research on Parkinson's disease and type 2 diabetes[1].
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VU0453379 | 98.0% | VU0453379 is a blood-brain barrier permeable GLP-1R positive allosteric modulator (PAM) with an EC50 value of 1.3 μM. VU0453379 potentiates the actions of endogenous GLP-1 and synthetic peptide agonists, and promotes GLP-1 receptor internalization. VU0453379 stimulates insulin secretion from primary mouse islets. VU0453379 enhances the function of endogenous GLP-1R and reverses catalepsy in animal models. VU0453379 is useful for research on Parkinson's disease and type 2 diabetes. | ||||||||||||||||||||
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- [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. [Content Brief]
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