KB-5492 free base

SKU: orb1687648

Description

KB-5492 free base is a selective sigma receptor antagonist, demonstrated by its inhibition of [³H]DTG binding, with oral bioavailability. It serves as a research tool for investigating gastric secretion and ulcerative lesions in both in vitro and in vivo experimental models.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 113594-64-2
• MW: 430.49
• Purity: 97.10% (May vary between batches)
• Formula: C₂₃H₃₀N₂O₆
• SMILES: COc1ccc(OC(=O)CN2CCN(Cc3cc(OC)c(OC)c(OC)c3)CC2)cc1
• Target: Sigma receptor
• Solubility: DMSO:80 mg/mL (185.83 mM)

Bioactivity

• Target IC50:
  σ receptor (DTG site):3.15 μM
• In Vivo:
  In male Sprague-Dawley rats weighing 210-240 g, induction of gastric mucosal damage was reduced by KB-5492 free base (200 mg/kg; oral gavage) compared to the control group. Additionally, it prevented deep mucosal lesions and exfoliation of surface epithelial cells.
• In Vitro:
  KB-5492 free base selectively inhibited specific [3H]1,3-di(2-tolyl)guanidine (DTG) binding to the sigma receptor (IC50 = 3.15 microM) with a pseudo-Hill coefficient of 0.33.

Storage & Handling

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

Alternative Names

Sigmareceptor, Sigma receptor

Compound Identifiers

PubChem CID

131083