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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 |
|---|
| Dulaglutide (Activated main chain)
Dulaglutide (Activated main chain) is a glucagon-like peptide-1 receptor agonist (GLP-1 agonist) consisting of GLP-1(7-37) covalently linked to an Fc fragment of human IgG4. |
| Shanzhiside-methylester
Shanzhiside Methyl ester was isolated from Lactobacillus rotaformis. Shanzhiside Methyl ester, a small molecule glucagon-like peptide 1 (GLP-1 receptor) agonist, has the ability to induce anti-abnormal pain tolerance. |
| Tirzepatide hydrochloride
Tirzepatide Hydrochloride is a glucose-dependent insulin-stimulating peptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist. |
| PF-07081532
PF-07081532 is a next-generation orally active GLP-1 receptor agonist. |
| BETP
BETP is an agonist of glucagon-like peptide-1 (GLP-1) receptor, with EC50s of 0.66 and 0.755 μM for human and rat GLP-1 receptor, respectively. |
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