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KB-5492 anhydrous

CAS: 129200-10-8 F: C27H34N2O10 W: 546.57

KB-5492 anhydrous is a potent and selective inhibitor of sigma receptor, inhibits specific 1,3-di(2-tolyl)guanidine (DTG
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Bioactivity 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].
Target IC50: 3.15 μM (sigma receptor)
Invitro 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:
Name KB-5492 anhydrous
CAS 129200-10-8
Formula C27H34N2O10
Molar Mass 546.57
Appearance Solid
Transport Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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.