| Identification | Back Directory | [Name]
VU0453379 | [CAS]
1638646-27-1 | [Synonyms]
VU0453379
1H-Pyrido[3,4-b]indole-4-carboxamide, 2-cyclopentyl-2,9-dihydro-9-methyl-N-[[(2S)-1-(1-methylethyl)-2-pyrrolidinyl]methyl]-1-oxo- | [Molecular Formula]
C26H34N4O2 | [MDL Number]
MFCD28502156 | [MOL File]
1638646-27-1.mol | [Molecular Weight]
434.57 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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,M59.2% 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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| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
|