L-168049

SKU: orb1704440

Description

L-168049 is a potent, selective, and non-competitive antagonist of the human glucagon receptor, exhibiting IC₅₀ values of 3.7 nM (human), 63 nM (murine), and 60 nM (canine). It is a valuable research tool for studying glucose metabolism and diabetes pathophysiology in both in vitro assays and in vivo models.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 191034-25-0
• MW: 467.79
• Purity: 99.87% (May vary between batches)
• Formula: C₂₄H₂₀BrClN₂O
• SMILES: CCCOc1ccc(Br)cc1-c1cc([nH]c1-c1ccncc1)-c1ccc(Cl)cc1
• Target: Glucagon Receptor
• Solubility: Ethanol:3.4 mM;DMSO:insoluble

Bioactivity

• Target IC50:
  Glucagon receptor (human):3.7 nM (IC50)|Glucagon receptor (murine):63 nM (IC50)|Glucagon receptor (canine):60 nM (IC50)
• In Vivo:
  In the liver of L-G6pc-/- mice, L-168049 (50 mg/kg body; p.o.) reduces Pck1 mRNA expression by half within 6 hours. L-168049 prevents the increase in G6pc expression in the kidney and gut .
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• In Vitro:
  In Chinese hamster ovary cells expressing the human glucagon receptor, L-168049 increases the apparent EC50 of glucagon-stimulated adenylate cyclase and decreases maximal glucagon stimulation with a Kb of 25 nM. L-168049 blocks glucagon-stimulated cAMP formation in mouse liver membrane and inhibits glucagon (100 pM)-stimulated cAMP synthesis in CHO cells expressing the human glucagon receptor with IC50 of 41 nM .
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Storage & Handling

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

Alternative Names

L-168,049, L168049, L-168049, human glucagon receptor, GlucagonReceptor, Glucagon Receptor, L 168049

Compound Identifiers

PubChem CID

5311276