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GRA Ex-25

Cat. No. M8940
GRA Ex-25 Structure
Size Price Availability Quantity
5mg USD 166.5  USD185 In stock
10mg USD 234  USD260 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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.

Protocol
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 563.61
Formula C29H36F3N3O5
CAS Number 307983-31-9
Purity >98%
Solubility DMSO: ≥ 20 mg/mL
Storage at -20°C
References

Glucagon receptor antagonism induces increased cholesterol absorption.
Guan HP, et al. J Lipid Res. 2015 Nov;56(11):2183-95. PMID: 26373568.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: GRA Ex-25 supplier, Glucagon Receptor, inhibitors

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