129200-10-8

129200-10-8 structure

Name: KB-5492 anhydrous
Chemical Name: but-2-enedioic acid,(4-methoxyphenyl) 2-[4-[(3,4,5-trimethoxyphenyl)methyl]piperazin-1-yl]acetate
CAS Number: 129200-10-8
Molecular Formula: C₂₇H₃₄N₂O₁₀
Molecular Weight: 546.56600
Catalog: Signaling Pathways GPCR/G Protein Sigma Receptor
Create Date: 2016-02-11 00:11:42
Modify Date: 2024-01-09 13:39:56
KB-5492 anhydrous 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 anhydrous is an anti-ulcer agent[1][2].

Name	but-2-enedioic acid,(4-methoxyphenyl) 2-[4-[(3,4,5-trimethoxyphenyl)methyl]piperazin-1-yl]acetate

Description	KB-5492 anhydrous 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 anhydrous is an anti-ulcer agent[1][2].
Related Catalog	Research Areas >> Inflammation/Immunology Signaling Pathways >> GPCR/G Protein >> Sigma Receptor
Target	IC50: 3.15 μM (sigma receptor)[1]
In Vitro	KB-5492 (0.001-100 μM) inhibits specific [3H]DTG binding in a concentration-dependent manner[1]. KB-5492 (0.1-1 mM) 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.) 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.