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Ezatiostat
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Ezatiostat图片
CAS NO:168682-53-9
包装:100 mg
市场价:6498元

产品名称
TER199(free base)
TLK199
产品介绍
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。

产品描述

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

体内活性

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].

Cas No.

168682-53-9

分子式

C27H35N3O6S

分子量

529.65

别名

TER199(free base);TLK199

储存和溶解度

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