KB-5492 free base 是一种有效的和选择性的sigma受体抑制剂,抑制 [3H]1,3-di(2-tolyl)guanidine (DTG) 与sigma受体结合,IC50值为 3.15 μM。KB-5492 free base 是一种抗溃疡剂。
产品描述
KB-5492 free base is a potent and selective inhibitor of sigma receptor, inhibits specific [ 3 H]1,3-di(2-tolyl)guanidine (DTG) binding to the sigma receptor with an IC 50 of 3.15 μM. KB-5492 free base is an anti-ulcer agent [1] [2].
体外活性
KB-5492 (0.001-100 μM) free base inhibits specific [ 3 H]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 51 Cr release from gastric epithelial cells [2].
体内活性
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.
Cas No.
113594-64-2
分子式
C23H30N2O6
分子量
430.49
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years