| Identification | Back Directory | [Name]
PF-06882961 | [CAS]
2230198-02-2 | [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
(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
1H-Benzimidazole-6-carboxylic acid, 2-[[4-[6-[(4-cyano-2-fluorophenyl)methoxy]-2-pyridinyl]-1-piperidinyl]methyl]-1-[(2S)-2-oxetanylmethyl]- | [Molecular Formula]
C31H30FN5O4 | [MDL Number]
MFCD32661373 | [MOL File]
2230198-02-2.mol | [Molecular Weight]
555.6 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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. | [storage]
Store at -20°C |
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