EzatioSTAT 是一种谷胱甘肽的三肽类似物，也是一种选择性的口服活性的谷胱甘肽 S-转移酶 P1-1 (GSTP1) 抑制剂。它通过抑制GSTP1导致 JNK 激活，刺激淋巴细胞生成和骨髓祖细胞增殖，可研究骨髓增生异常综合症。

Ezatiostat is a tripeptide analog of glutathione that can selectively inhibit GSTP1-1 catalytic activity.

Ezatiostat was administered to 19 patients with non-deletion(5q) myelodysplastic syndrome (MDS) at one of two doses (2000 mg or 2500 mg/day) in combination with 10 mg of lenalidomide on days 1-21 of a 28-day cycle. One of 4 evaluable patients (25%) in the 2500/10 mg dose group experienced an erythroid hematologic improvement (HI-E) response by 2006 MDS International Working Group (IWG) criteria. Four of 10 evaluable patients (40%) in the 2000 mg/10 mg dose group experienced a HI-E response [1]. Systemic inhibition of GSTP1 with Ezatiostat (0-30 mg/kg, i.p.) dose-dependently reduced the reinforcing effects of alcohol as measured by operant self-administration, in the absence of motor effects [2].

168682-53-9

C27H35N3O6S

529.65

TER199(free base);TLK199

H2O:Insoluble
DMSO:>50 mg/mL (94.4 mM)
Ethanol:20 mg/mL (37.76)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years