129200-10-8
中文名稱(chēng)
KB 5492
英文名稱(chēng)
KB 5492
CAS
129200-10-8
分子式
C27H34N2O10
分子量
546.57
MOL 文件
129200-10-8.mol
129200-10-8 結(jié)構(gòu)式
常見(jiàn)問(wèn)題列表
生物活性
KB-5492 anhydrous 是一種有效的和選擇性的 sigma 受體抑制劑，抑制 [3H]1,3-di(2-tolyl)guanidine (DTG) 與 sigma 受體結(jié)合，IC50 值為 3.15 μM。KB-5492 anhydrous 是一種抗?jié)兯帯?/span>靶點(diǎn)
IC50: 3.15 μM (sigma receptor)
體外研究
KB-5492 (0.001-100 μM) inhibits specific [
3
H]DTG binding in a concentration-dependent manner.
KB-5492 (0.1-1 mM) significantly and concentration-dependently prevents the ethanol- and acidified aspirin-induced increases in
51
Cr release from gastric epithelial cells.
體內(nèi)研究
KB-5492 (200?mg/kg; p.o.) prevents macroscopic lesions in the gastric mucosa.
| Animal Model: | Male Sprague-Dawley rats weighing 210-240 g are induced gastric mucosal damage |
| 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. |