All AbMole products are for research use only, cannot be used for human consumption.
Danuglipron (PF-06882961) is a potent, orally bioavailable agonist of the glucagon-like peptide-1 receptor (GLP-1R) agonist. PF-06882961 stimulates cAMP accumulation in CHO cells expressing both the human and monkey GLP-1Rs with comparable EC50 values. PF-06882961 shows mild to moderate damage to the heart, moderate to severe effects on the thymus gland (which helps with managing infection), mild to moderate stomach ulcers at the highest dose level given in the rat.
| Cell Experiment | |
|---|---|
| Cell lines | HEK293 cells |
| Preparation 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. |
| Concentrations | 1 μM |
| Incubation time | 30 minutes |
| Animal Experiment | |
|---|---|
| Animal models | male Wistar-Han rats / cynomolgus monkeys |
| Formulation | - |
| Dosages | 1 mg/kg iv; 5 mg/kg, 100 mg/kg PO |
| Administration | iv, PO |
| Molecular Weight | 555.6 |
| Formula | C31H30FN5O4 |
| CAS Number | 2230198-02-2 |
| Solubility (25°C) | DMSO 10 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related GLP Receptor Products |
|---|
| V-0219 hydrochloride
V-0219 hydrochloride is an orally active, positive allosteric modulator (PAM) of the glucagon-like peptide-1 receptor (GLP-1R). |
| GLP-1 receptor agonist 14
GLP-1 receptor agonist 14 is a potent agonist of glucagon-like peptide-1 (GLP-1). |
| NM-003
NM-003 is a GLP-2R agonist that can be used in studies related to inflammatory bowel disease. |
| NB-1002
NB-1002 is a GLP-2R agonist that can be used in studies related to short bowel syndrome. |
| MOD-15014
MOD-15014 is a GLP-2R modulator that can be used in studies related to short bowel syndrome. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2024 AbMole BioScience. All Rights Reserved.
