KB-5492 anhydrous

Modify Date: 2024-01-09 13:39:56

KB-5492 anhydrous Structure
KB-5492 anhydrous structure
Common Name KB-5492 anhydrous
CAS Number 129200-10-8 Molecular Weight 546.56600
Density N/A Boiling Point 553.2ºC at 760 mmHg
Molecular Formula C27H34N2O10 Melting Point N/A
MSDS N/A Flash Point 288.3ºC

 Use of KB-5492 anhydrous


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].

 Names

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

 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
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
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