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.
|Animal models||Non-fasted male Sprague Dawley rats (200 g)|
|Dosages||0, 1, 3, 10 and 30 mg/kg|
|Administration||acatheter inserted in a jugular vein|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO: ≥ 20 mg/mL|
Glucagon receptor antagonism induces increased cholesterol absorption.
Guan HP, et al. J Lipid Res. 2015 Nov;56(11):2183-95. PMID: 26373568.
|Related Glucagon Receptor Products|
PF-06291874 is an orally active, potent and selective glucagon receptor antagonist.
Dulaglutide 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.
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