KB-5492 free base_product_DataBase

Bioactivity

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].

Target

IC50: 3.15 μM (sigma receptor)

Invitro

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:

Name

KB-5492 free base

CAS

113594-64-2

Formula

C23H30N2O6

Molar Mass

430.49

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[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.

PeptideDB

KB-5492 free base

CAS: 113594-64-2 F: C23H30N2O6 W: 430.49