Home GPCR & G Protein Glucagon Receptor agonist Danuglipron (PF-06882961) For research use only.

Danuglipron (PF-06882961)

Danuglipron (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.

Danuglipron (PF-06882961) Chemical Structure

Danuglipron (PF-06882961) Chemical Structure

CAS: 2230198-02-2

Purity & Quality Control

Batch: Purity: 99.87%
99.87

Danuglipron (PF-06882961) Related Products

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Biological Activity

Description Danuglipron (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.
Targets
GLP-1 receptor [1]
In vitro
In vitro

PF-06882961 stimulates cAMP accumulation in CHO cells expressing both the human and monkey GLP-1Rs with comparable EC50 values. In contrast, PF-06882961 does not increase cAMP levels in cells expressing the mouse, rat, or rabbit GLP-1R.[2]
Cell Research Cell lines HEK293 cells
Concentrations 1 μM
Incubation Time 30 minutes
Method

HEK293 cells stably expressing hGLP-1R fused to green fluorescent protein (GFP) (400,000 cells per well) are cultured onto 6 well plates for 24 hours and stimulated with PF-06882961 for 30 minutes. An agonist concentration of 1 μM shown to induce maximal internalization is chosen for these studies. In selected wells, cells are washed three times with PBS containing 0.1 % BSA and incubated at 37 °C for an additional 2 hours to assess reversibility of the endocytosis process. Cells are then fixed with 4% paraformaldehyde for 15 minutes at room temperature followed by three washes with PBS containing 0.1% BSA.
In Vivo
In vivo

PF-06882961 potentiates glucose-stimulated insulin release and reduces food intake in monkeys.[2]
Animal Research Animal Models male cynomolgus monkeys
Dosages 1 mg/kg, 5 mg/kg, 100 mg/kg
Administration IV, Oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04552470 Completed
Type 2 Diabetes Mellitus
Pfizer
 October 26 2020 Phase 1
NCT03538743 Completed
Type 2 Diabetes Mellitus
Pfizer
 June 25 2018 Phase 1

Chemical Information & Solubility

Molecular Weight 555.60 Formula

C31H30FN5O4
CAS No. 2230198-02-2 SDF --
Smiles OC(=O)C1=CC=C2N=C(CN3CCC(CC3)C4=NC(=CC=C4)OCC5=C(F)C=C(C=C5)C#N)[N](CC6CCO6)C2=C1
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

Ethanol : 100 mg/mL

DMSO : 10 mg/mL ( (17.99 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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