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KB-5492 anhydrous

Names

[ CAS No. ]:
129200-10-8

[ Name ]:
KB-5492 anhydrous

Biological Activity

[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.

Chemical & Physical Properties

[ Boiling Point ]:
553.2ºC at 760 mmHg

[ Molecular Formula ]:
C27H34N2O10

[ Molecular Weight ]:
546.56600

[ Flash Point ]:
288.3ºC

[ Exact Mass ]:
546.22100

[ PSA ]:
144.30000

[ LogP ]:
2.03180

[ Vapour Pressure ]:
2.8E-12mmHg at 25°C

Related Compounds