Acivicin (hydrochloride)
中文名:盐酸阿西维辛
CAS:161922-40-3
品牌:MedChemExpress (MCE)
存储条件:4°C, stored under nitrogen
生物活性:Acivicin hydrochloride (AT-125 hydrochloride) 是 Streptomyces sviceus 产生的天然产物,是一种 γ-谷氨酰转肽酶 (GGT) 抑制剂。 Acivicin hydrochloride 可以穿过血脑屏障,具有抗癌、抗寄生虫的特性[1][2]。 IC50 和目标:γ-谷氨酰转肽酶[1]
体外:Acivicin hydrochloride(AT-125 盐酸盐;0.1-50 μM;5 天)在人 HepG2 细胞[1] 中的 IC50 为 0.7 μM。
体内:Acivicin hydrochloride(AT-125 hydrochloride;5 mg/kg;IP;每周两次)将尿 γ-GT 降低 70-78%[3]。
参考文献:
[1]. Delphine Waniusiow, et al. Toluene-induced hearing loss in acivicin-treated rats. Neurotoxicol Teratol. May-Jun 2008;30(3):154-60.
[2]. Kreuzer J, et al. Target discovery of acivicin in cancer cells elucidates its mechanism of growth inhibition. Chem Sci. 2014 Dec 1;6(1):237-245. Epub 2014 Sep 26.
[3]. Chikhale EG, et al. Carrier-mediated transport of the antitumor agent acivicin across the blood-brain barrier. Biochem Pharmacol. 1995 Mar 30;49(7):941-5.