| Identification | Back Directory | [Name]
Benzeneacetic acid, 2-[1-[(1R)-1-(2,6-dichloro-3-cyclopropylphenyl)ethyl]-1H-imidazo[4,5-c]pyridin-6-yl]-α-methyl-, (αR)- | [CAS]
2764704-18-7 | [Synonyms]
Benzeneacetic acid, 2-[1-[(1R)-1-(2,6-dichloro-3-cyclopropylphenyl)ethyl]-1H-imidazo[4,5-c]pyridin-6-yl]-α-methyl-, (αR)- | [Molecular Formula]
C26H23Cl2N3O2 | [MOL File]
2764704-18-7.mol | [Molecular Weight]
480.39 |
| Chemical Properties | Back Directory | [Boiling point ]
665.3±65.0 °C(Predicted) | [density ]
1.41±0.1 g/cm3(Predicted) | [solubility ]
Acetonitrile: Slightly soluble: 0.1-1 mg/ml DMSO: Sparingly soluble: 1-10 mg/ml | [form ]
Solid | [pka]
4.16±0.10(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Description]
LSN3318839 is a positive allosteric modulator (PAM) of glucagon-like peptide 1 receptor (GLP-1R).1 It potentiates increases in cAMP accumulation induced by the GLP-1R full agonist GLP-1 (9-36), but not the GLP-1R partial agonist GLP-1 (7-36), in INS-1 832/3 cells. LSN3318839 (1 and 3 µM) increases insulin levels in the presence, but not absence, of GLP-1 (9-36) in INS-1 832/3 cells under high-glucose conditions. It reduces blood glucose levels in glucose-dependent insulinotropic polypeptide receptor (GIPR) knockout mice in an oral glucose tolerance test when administered at a dose of 30 mg/kg and has an additive effect on reducing blood glucose levels in GIPR knockout mice when administered at 10 or 30 mg/kg in combination with the dipeptidyl peptidase 4 (DPP-4) inhibitor sitagliptin.WARNING This product is not for human or veterinary use. | [References]
[1] FRANCIS S. WILLARD. Discovery of an Orally Efficacious Positive Allosteric Modulator of the Glucagon-like Peptide-1 Receptor[J]. Journal of Medicinal Chemistry, 2021, 64 6: 3439-3448. DOI: 10.1021/acs.jmedchem.1c00029 |
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