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| | PF-06882961 Basic information |
| Product Name: | PF-06882961 | | Synonyms: | PF-06882961;PF-06882961;PF 06882961;PF06882961;2-[[4-[6-[(4-CYANO-2-FLUOROPHENYL)METHOXY]PYRIDIN-2-YL]PIPERIDIN-1-YL]METHYL]-3-[[(2S)-OXETAN-2-YL]M;1H-Benzimidazole-6-carboxylic acid, 2-[[4-[6-[(4-cyano-2-fluorophenyl)methoxy]-2-pyridinyl]-1-piperidinyl]methyl]-1-[(2S)-2-oxetanylmethyl]-;(S)-2-((4-(6-((4-cyano-2-fluorobenzyl)oxy)pyridin-2-yl)piperidin-1-yl)methyl)-1-(oxetan-2-ylmethyl)-1H-benzo[d]imidazole-6-carboxylic acid;Danuglipron (PF-06882961);2-[[4-[6-[(4-Cyano-2-fluorophenyl)methoxy]-2-pyridinyl]-1-piperidinyl]methyl]-1-[(2S)-2-oxetanylmethyl]-1H-benzimidazole-6-carboxylic acid;PF 06882961,PF06882961 | | CAS: | 2230198-02-2 | | MF: | C31H30FN5O4 | | MW: | 555.6 | | EINECS: | | | Product Categories: | API | | Mol File: | 2230198-02-2.mol |  |
| | PF-06882961 Chemical Properties |
| Boiling point | 782.6±60.0 °C(Predicted) | | density | 1.39±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO:10.0(Max Conc. mg/mL);18.0(Max Conc. mM)
Ethanol:100.0(Max Conc. mg/mL);179.98(Max Conc. mM) | | form | Solid powder | | pka | 3.41±0.30(Predicted) | | InChIKey | HYBAKUMPISVZQP-DEOSSOPVSA-N | | SMILES | C1(CN2CCC(C3=NC(OCC4=CC=C(C#N)C=C4F)=CC=C3)CC2)N(C[C@@H]2CCO2)C2=CC(C(O)=O)=CC=C2N=1 |
| | PF-06882961 Usage And Synthesis |
| Uses | PF-06882961 is a potent, orally bioavailable glucagon-like peptide-1 receptor agonist (GLP-1R) agonist. It has blood glucose lowering and weight loss properties and is used to treat type 2 diabetes (T2D) and obesity. | | in vitro | For example, a methylene-linked oxetane increased potency ~100-fold relative to the methyl substituent of 5, leading to the
identification of PF-06882961, which is a full agonist (EC50 = 13 nM) in the CS cAMP assay. PF-06882961 also
incorporates a nitrile replacement for the chloride in the benzyl ether region, which served to reduce CLint in HLM as well as in
human hepatocytes.
Reference: J Med Chem. 2022 Jun 23;65(12):8208-8226. https://pubmed.ncbi.nlm.nih.gov/35647711/ | | in vivo | Intravenous infusion of PF-06882961 during the IVGTT led to an increase in insulin secretion and the rate of glucose disappearance
(K-value). Enhancement of glucose-stimulated insulin secretion by PF-06882961 was concentration-dependent and was
also observed following oral dosing with similar efficacy when compared to administration by IV infusion. Once-daily
administration of PF-06882961 for 2 days also inhibited food intake compared to vehicle-treated monkeys.
Reference: J Med Chem. 2022 Jun 23;65(12):8208-8226. https://pubmed.ncbi.nlm.nih.gov/35647711/
| | target | PF-06882961, a non-peptide agonist, activates the canonical G protein signaling activity only in the Glucagon-like
peptide-1 (GLP-1) receptor with Trp33ECD. |
| | PF-06882961 Preparation Products And Raw materials |
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