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Chemical Structure : V-0219
Catalog No.: PC-72853Not For Human Use, Lab Use Only.
V-0219 is a small molecule positive allosteric modulator (PAM) of GLP-1R with Emax of 60% in the cAMP assay.
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V-0219 is a small molecule positive allosteric modulator (PAM) of GLP-1R with Emax of 60% in the cAMP assay.
V-0219 potentiated insulin secretion in INS-1 β-cells with EC50 of 0.25 nM, the best response was observed at 0.1 nM, when a fixed concentration of 0.2 nM of GLP-1 was added to the dose-response curve of 9, the maximal response observed reached a plateau at 0.1 nM, with an EC50 value of 0.008 nM.
V-0219 shows a remarkable in vivo activity, reducing food intake and improving glucose handling in normal and diabetic rodents.
| M.Wt | 410.441 | |
| Formula | C20H25F3N4O2 | |
| Appearance | Solid | |
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1. Juan M. Decara, et al. Journal of Medicinal Chemistry. DOI: 10.1021/acs.jmedchem.1c01842
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