PF-06882961 Property

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)

color 

Off-white to light yellow

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 and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

PF-06882961 Chemical Properties,Usage,Production

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.