CAS NO: | 152684-53-2 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
生物活性 | TLK117, the active metabolite of TLK199, selective inhibitsGlutathione S-transferase P1–1 (GSTP1-1)with aKiof 0.4 μM for GSTP. TLK117 also competitively inhibitsglyoxalaseIwith aKiof 0.56 μM. | ||||||||||||||||
IC50& Target | Ki: 0.4 μM[1], 0.56 μM (glyoxalase I)[2] | ||||||||||||||||
体外研究 (In Vitro) | TLK117 is the most specific GSTP inhibitor to date, with a binding affinity greater than GSH itself and a selectivity for GSTP over 50-fold greater than the GSTM and GSTA classes (Ki=0.4 μM)[1]. TER 117 is developed as a GST P1-1 isoenzyme inhibitor to circumvent the indicated contribution of GST P1-1 to drug resistance of tumor cells. To facilitate the cellular uptake of TER 117, it is delivered as a diethyl ester (TER 117 DEE, also called TER 199). TER 117 is found to be a competitive inhibitor of both GST P1-1 and glyoxalase I[2]. | ||||||||||||||||
体内研究 (In Vivo) | Oropharyngeal administration of the GSTP inhibitor, TLK117, at a time when fibrosis is already apparent, attenuated bleomycin- and AdTGFβ-induced remodeling, α-SMA, caspase activation, FAS S-glutathionylation, and total protein S-glutathionylation. Four hours after administration of 50 mg/kg TLK117, GSTP activity is strongly decreased and remains decreased by about 60% for at least 24 hours[2]. | ||||||||||||||||
分子量 | 473.54 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C23H27N3O6S | ||||||||||||||||
CAS 号 | 152684-53-2 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
| ||||||||||||||||
溶解性数据 | In Vitro: DMSO : 150 mg/mL(316.76 mM;Need ultrasonic) 配制储备液
* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百
|