113594-64-2

113594-64-2 structure
113594-64-2 structure
  • Name: KB-5492 free base
  • Chemical Name: KB-5492 free base
  • CAS Number: 113594-64-2
  • Molecular Formula: C23H30N2O6
  • Molecular Weight: 430.49
  • Catalog: Signaling Pathways GPCR/G Protein Sigma Receptor
  • Create Date: 2022-08-07 11:28:51
  • Modify Date: 2024-01-09 11:19:21
  • KB-5492 free base is a potent and selective inhibitor of sigma receptor, inhibits specific [3H]1,3-di(2-tolyl)guanidine (DTG) binding to the sigma receptor with an IC50 of 3.15 μM. KB-5492 free base is an anti-ulcer agent[1][2].

Name KB-5492 free base
Description KB-5492 free base is a potent and selective inhibitor of sigma receptor, inhibits specific [3H]1,3-di(2-tolyl)guanidine (DTG) binding to the sigma receptor with an IC50 of 3.15 μM. KB-5492 free base is an anti-ulcer agent[1][2].
Related Catalog
Target

IC50: 3.15 μM (sigma receptor)[1]

In Vitro KB-5492 (0.001-100 μM) free base inhibits specific [3H]DTG binding in a concentration-dependent manner[1]. KB-5492 (0.1-1 mM) free base significantly and concentration-dependently prevents the ethanol- and acidified aspirin-induced increases in 51Cr release from gastric epithelial cells[2].
In Vivo KB-5492 (200 mg/kg; p.o.) free base prevents macroscopic lesions in the gastric mucosa[2]. Animal Model: Male Sprague-Dawley rats weighing 210-240 g are induced gastric mucosal damage[2] Dosage: 200 mg/kg Administration: Oral gavage Result: Reduced the lesion length as compared with the control. Prevented the deep mucosal lesions and exfoliation of surface epithelial cells.
References

[1]. Harada Y, et, al. Receptor binding profiles of KB-5492, a novel anti-ulcer agent, at sigma receptors in guinea-pig brain. Eur J Pharmacol. 1994 May 2; 256(3): 321-8.

[2]. Morimoto Y, et, al. Effects of KB-5492, a new anti-ulcer agent, on ethanol- and acidified aspirin-induced gastric mucosal damage in vivo and in vitro. Jpn J Pharmacol. 1994 Jan; 64(1): 41-7.

Molecular Formula C23H30N2O6
Molecular Weight 430.49