Free shipping on all orders over $ 500
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 | cynomolgus monkeys |
| Formulation | - |
| Dosages | 1 mg/kg iv; 5 mg/kg, 100 mg/kg PO |
| Administration | iv, PO |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Molecular Weight | 555.6 |
| Formula | C31H30FN5O4 |
| CAS Number | 2230198-02-2 |
| Purity | >99% |
| Solubility | DMSO 100 mg/mL |
| Storage | at -20°C |
| Related Glucagon Receptor Products |
|---|
| LSN3318839
LSN3318839 is an orally active allosteric modulator of glucagon-like peptide-1 receptor (GLP-1R). |
| GLP-1(7-36), amide TFA
TFA is a major intestinal hormone that stimulates insulin secretion by pancreatic beta cells in response to glucose. |
| GLP-1(7-37)
Glp-1 (7-37) is an intestinal insulin hormone that enhances glucose-induced insulin secretion. |
| Teduglutide
Teduglutide is a glucagon-like peptide-2 (GLP- 2) receptor agonist used for the treatment of short-bowel syndrome. |
| NNC0640
NNC0640 is a potent, negative allosteric modulator (NAM) of human G-protein-coupled glucagon receptor (GCGR) with IC50 of 69.2 nM. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.
