GRA Ex-25

SKU: orb1304215

Description

GRA Ex-25 (GRA-Ex-25) is a small molecule antagonist of the glucagon receptor (GCGR). It is a valuable research tool for studying glucose metabolism and diabetes pathophysiology in both cellular assays and animal models.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 307983-31-9
• MW: 563.61
• Purity: 97.39% (May vary between batches)
• Formula: C₂₉H₃₆F₃N₃O₅
• SMILES: CC(C)(C)[C@H]1CC[C@@H](CC1)N(Cc1ccc(cc1)C(=O)NCCC(O)=O)C(=O)Nc1ccc(OC(F)(F)F)cc1
• Target: Glucagon Receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.55 mM);DMSO:50 mg/mL (88.71 mM)

Bioactivity

• Target IC50:
  Glucagon (human):55 nM|Glucagon (rat):56nM
• In Vivo:
  GRA Ex-25 (3 mg/kg, i.v.) significantly reduces blood glucose induced by exogenous glucagon in rat models, likely through direct inhibition of glucagon-stimulated hepatic glucose output.
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• In Vitro:
  GRA Ex-25 binds to the human glucagon receptor (h-GlucRbind) with a Ki of 63 nM and exhibits moderate glucagon-induced adenylate cyclase inhibition (h-GlucRcyclase) with a Ki of 254 nM under our assay conditions, showing similar affinity for both rat and human glucagon receptors (IC50=56 and 55 nM, respectively).
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GCGR, Glucagon Receptor, GlucagonReceptor, GRA Ex 25, GRA Ex25, GRA Ex-25, GRA-Ex-25, human glucagon receptor, inhibit, Inhibitor, rat glucagon receptor

Compound Identifiers

PubChem CID

16100296