Sograzepide

SKU: orb1706618

Description

Sograzepide (Netazepide) is a potent, selective, and orally bioavailable gastrin/CCK-B receptor antagonist. It suppresses gastrin-mediated signaling and pappalysin 2 expression, demonstrating the ability to induce regression of type 1 gastric neuroendocrine tumors (gNETs) in clinical research. This small molecule is a valuable tool for investigating gastrin biology and gNET pathogenesis in both in vitro and in vivo models.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 155488-25-8
• MW: 498.58
• Formula: C₂₈H₃₀N₆O₃
• SMILES: C(C(C(C)(C)C)=O)N1C=2C(C(=N[C@@H](NC(NC3=CC(NC)=CC=C3)=O)C1=O)C4=CC=CC=N4)=CC=CC2
• Target: Cholecystokinin Receptor,Others
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (6.62 mM);DMSO:80 mg/mL (160.46 mM)

Bioactivity

• Target IC50:
  Gastrin/CCK-B:0.1 nM|Gastrin/CCK-A:501 nM
• In Vivo:
  Intravenous Sograzepide (0.1 μmol/kg) inhibited gastrin-induced gastric acid secretion in anesthetized rats at a dose of ED50 = 87 nM/kg. At a dose of 10 μM/kg, Sograzepide showed inhibition of gastrin-induced gastric acid secretion with an ED50 = 0.0086 μM/kg, but had no effect on histamine- and bethanechol-induced gastric acid secretion.

Storage & Handling

• Storage: store at low temperature | Pure form: -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

Sograzepide, YM 220, YF476, YF-476, YF 476, YM220, YM-220, Netazepide, Gastrin, Gastrin/CCK-A, Gastrin/CCK-B

Compound Identifiers

PubChem CID

9870520