货号	规格	价格	上海	北京	珠海	重庆	武汉
S83862-5mg买3赠1	98.30%	￥440.00 S83862-5mg ￥440.00 现货（买3赠1）	6 6	-	-	-	-
S83862-10mg买3赠1	98.30%	￥660.00 S83862-10mg ￥660.00 现货（买3赠1）	5 5	-	-	-	-
S83862-50mg	98.30%	￥2550.00 S83862-50mg ￥2550.00 现货	1 1	-	-	-	-
S83862-100mg	≥96%	￥3820.00 S83862-100mg ￥3820.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

Ezatiostat (TER199 free base; TLK199) is a tripeptide analog of glutathione and is a selective and orally active glutathione S-transferase P1-1 (GSTP1) inhibitor. Ezatiostat leads to JNK activation by inhibiting GSTP1. Ezatiostat stimulates both lymphocyte production and bone marrow progenitor proliferation. Ezatiostat has the potential for myelodysplastic syndrome (MDS) treatment

靶点：

Glutathione S-transferase P1-1 (GSTP1);Apoptosis; GlutathionePeroxidase; GST

体外研究：

Ezatiostat causes dissociation of the enzyme from the jun-N-terminal kinase/c-Jun (JNK/JUN) complex, leading to JNK activation by phosphorylation. The therapeutic action of ezatiostat appears to include both proliferation of normal myeloid progenitors as well as apoptosis of the malignant clone.
Selection of a resistant clone of an HL60 tumor cell line through chronic exposure to Ezatiostat (TLK199) results in cells with elevated activities of c-Jun NH2 terminal kinase (JNK1) and ERK1/ERK2, and allowes the cells to proliferate under stress conditions that induced high levels of apoptosis in the wild type cells.

体内研究：

Administration of Ezatiostat (TLK199), stimulates both lymphocyte production and bone marrow progenitor (colony-forming unit-granulocyte macrophage) proliferation, but only in glutathione S-transferase P1-1 (GSTP1+/+) and not in GSTP1-/- animals.

参考文献：

1. Galili N, et al. Prediction of response to therapy with ezatiostat in lower risk myelodysplastic syndrome. J Hematol Oncol. 2012 May 6;5:20 2. Ruscoe JE, et al. Pharmacologic or genetic manipulation of glutathione S-transferase P1-1 (GSTpi) influences cell proliferation pathways. J Pharmacol Exp Ther. 2001 Jul;298(1):339-45.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.888 ml	9.44 ml	18.88 ml
5 mM	0.378 ml	1.888 ml	3.776 ml
10 mM	0.189 ml	0.944 ml	1.888 ml
50 mM	0.038 ml	0.189 ml	0.378 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

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Ezatiostat

(S)-ethyl 2-amino-5-(((R)-3-(benzylthio)-1-(((S)-2-ethoxy-2-oxo-1-phenylethyl)amino)-1-oxopropan-2-yl)amino)-5-oxopentanoate

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质检证书(COA)

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)