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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 |
|---|
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GLP-1R agonist is a potent GLP-1R (glucagon-like peptide 1 receptor) agonist, with KB of 26.3 nM for the recombinant human receptor. GLP-1R agonists play a key role in lowering glycated hemoglobin levels. It improves glycemic control and maintenance of body weight. |
| Glucagon (19-29), human
Glucagon (19-29), human is a potent and efficient inhibitor of insulin secretion. |
| Exendin-3/4 (59-86)
Exendin-3/4 (59-86) is a Exendin-4 peptide derivative. |
| HAEGTFTSDVS
HAEGTFTSDVS is the first N-terminal 1-11 residues of GLP-1 peptide. |
| GLP-1(32-36)amide
GLP-1(32-36)amide, a pentapeptide, derived from the C terminus of the glucoregulatory hormone GLP-1. |
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