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GRA Ex-25 is an inhibitor of glucagon receptor. GRA Ex-25 binds a human glucagon receptor (h-GlucRbind) with Ki of 63 nM and a moderate glucagon induced adenylate cyclase inhibition (h-GlucRcyclase) with Ki of 254 nM under our assay conditions.
In vivo: GRA Ex-25 (3 mg/kg, i.v.) significantly reduces blood glucose caused by exogenous administration of glucagon in rat model. GRA Ex-25 is able to inhibit the rise in blood glucose levels elicited by exogenous administered glucagon, most likely because of the direct inhibition of glucagon stimulated hepatic glucose output.
| Cell Experiment | |
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| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
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| Animal models | Non-fasted male Sprague Dawley rats (200 g) |
| Formulation | |
| Dosages | 0, 1, 3, 10 and 30 mg/kg |
| Administration | acatheter inserted in a jugular vein |
| Molecular Weight | 563.61 |
| Formula | C29H36F3N3O5 |
| CAS Number | 307983-31-9 |
| Solubility (25°C) | DMSO: ≥ 20 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Glucagon Receptor Products |
|---|
| PF-06291874
PF-06291874 is an orally active, potent and selective glucagon receptor antagonist. |
| Glucagon (1-29), bovine, human, porcine
Glucagon (1-29), bovine, human, porcine is a peptide hormone, produced by pancreatic α-cells. Glucagon stimulates gluconeogenesis. Glucagon (1-29), bovine, human, porcine activates HNF4α and increases HNF4α phosphorylation. |
| NNC0640
NNC0640 is a potent, negative allosteric modulator (NAM) of human G-protein-coupled glucagon receptor (GCGR) with IC50 of 69.2 nM. |
| Dasiglucagon acetate
Dasiglucagon acetate is a Glucagon Receptor Agonist. The physiologic effect of dasiglucagon is by means of Increased Glycogenolysis. |
| Adomeglivant
Adomeglivant (LY2409021) is a potent, selective glucagon receptor (GluR) allosteric antagonist. Adomeglivant is widely used in the research for type 2 diabetes mellitus. |
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