| Identification | Back Directory | [Name]
1-Piperazineacetic acid, 4-[(3,4,5-trimethoxyphenyl)methyl]-, 4-methoxyphenyl ester | [CAS]
113594-64-2 | [Synonyms]
1-Piperazineacetic acid, 4-[(3,4,5-trimethoxyphenyl)methyl]-, 4-methoxyphenyl ester | [Molecular Formula]
C23H30N2O6 | [MOL File]
113594-64-2.mol | [Molecular Weight]
430.49 |
| Chemical Properties | Back Directory | [Melting point ]
94-97 °C(Solv: ethyl ether (60-29-7); hexane (110-54-3)) | [Boiling point ]
553.2±50.0 °C(Predicted) | [density ]
1.176±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 100 mg/mL (232.29 mM; Need ultrasonic) | [form ]
Solid | [pka]
6.21±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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]. | [Biological Activity]
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].
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].
KB-5492 (200 mg/kg; p.o.) free base prevents macroscopic lesions in the gastric mucosa[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. |
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