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 | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| 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 |
| 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.
| Related Glucagon Receptor Products |
|---|
| 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. |
| HAEGTFTSD
HAEGTFTSD is a 9-residue peptide of human GLP-1 peptide or GLP-1(7-36), amide. |
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