BIIE-0246

SKU: orb1707553

Description

BIIE-0246 is a potent and selective antagonist of the NPY Y2 receptor, exhibiting an IC50 of 15 nM in rat binding assays. It effectively inhibits NPY-induced phosphorylation of AKT and MAPK signaling pathways, making it a valuable tool for investigating metabolic and neurological functions in both cellular and animal models.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 246146-55-4
• MW: 896.05
• Purity: 98.03% (May vary between batches)
• Formula: C₄₉H₅₇N₁₁O₆
• SMILES: O=C1C=2C(C(C=3C(N1)=CC=CC3)N4CCN(C(CC5(CC(N[C@H](C(NCCN6C(=O)N(N(C6=O)C7=CC=CC=C7)C8=CC=CC=C8)=O)CCCNC(=N)N)=O)CCCC5)=O)CC4)=CC=CC2
• Target: Neuropeptide Y Receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween-80+45% Saline:3.3 mg/mL (3.68 mM);DMSO:≥ 80 mg/mL

Bioactivity

• Target IC50:
  NPYY2 receptor:15±3 nM
• In Vivo:
  BIIE-0246 (10 μg/day, administered via intraperitoneal injection or subcutaneous osmotic minipump for 14 days) significantly reduced the urinary albumin-to-creatinine ratio (uACR) in the adriamycin nephropathy (AN) mouse model, ameliorated renal histopathological damage (such as glomerulosclerosis and reduced tubular casts), and markedly alleviated podocyte foot process effacement as confirmed by electron microscopy analysis .
• In Vitro:
  BIIE-0246 (1 µM, 24 hours) pretreatment significantly inhibited NPY-induced phosphorylation activation of Akt and MAPK in mouse podocytes .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AR-H 053591, AR-H053591, AR-H-053591, BIIE 0246, BIIE0246, BIIE-0246, NPYY2 receptor, plusmn

Compound Identifiers

PubChem CID

9811493