iGOT1-01
目录号: PL08359 纯度: ≥99%
iGOT1-01 是有效的天冬氨酸转氨酶 1 (谷氨酸草酰乙酸转氨酶 1;GOT1) 抑制剂,在 MDH 偶联 GOT1 酶法测定中 IC50 为 85 μM,在 GOT1/GLOX/HRP 测定中 IC50 为 11.3 μM。iGOT1-01 具有抗癌活性。
CAS No. :882256-55-5
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中文名称
iGOT1-01
英文名称
iGOT1-01
英文别名
Oprea1_534811;1-piperazinecarboxamide,4-(1h-indol-4-yl)-n-phenyl-;BDBM50462552;iGOT1-01
Cas No.
882256-55-5
分子式
C19H20N4O
分子量
320.39
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
iGOT1-01 是有效的天冬氨酸转氨酶 1 (谷氨酸草酰乙酸转氨酶 1;GOT1) 抑制剂,在 MDH 偶联 GOT1 酶法测定中 IC50 为 85 μM,在 GOT1/GLOX/HRP 测定中 IC50 为 11.3 μM。iGOT1-01 具有抗癌活性。
生物活性
iGOT1-01 is a potent aspartate aminotransferase 1 (glutamate oxaloacetate transaminase 1; GOT1) inhibitor. iGOT1-01 has IC 50 s of 85 μM and 11.3 μM in MDH coupled GOT1 enzymatic assay and GOT1/GLOX/HRP assay, respectively. iGOT1-01 has anti-cancer activity.
性状
Solid
IC50 & Target[1][2]
IC50: 85 μM (MDH coupled GOT1 enzymatic assay) and 11.3 μM (GOT1/GLOX/HRP assay)
体外研究(In Vitro)
iGOT1-01 has an IC50 of 84.6 μM in the GOT1/MDH1 assay. No inhibitory activity is observed for iGOT1-01 against MDH1 alone at 100 μM.
iGOT1-01 (3.125-200 μM; for 3 h) reveals little to no toxicity using two readouts of cell viability in PaTu8902 pancreatic and DLD1 colon cancer cells.
has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
iGOT1-01 (compound 1a; 20 mg/kg; oral) has reasonable bioavailability and exposure properties (t 1/2 =0.7 hours, C max =4133 ng/mL, AUC (0-24 hours) =11734 hour?ng/mL).
has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Justin Anglin, et al. Discovery and optimization of aspartate aminotransferase 1 inhibitors to target redox balance in pancreatic ductal adenocarcinoma. Bioorg Med Chem Lett. 2018 Sep 1;28(16):2675-2678.
[2]. Melissa C Holt, et al. Biochemical Characterization and Structure-Based Mutational Analysis Provide Insight into the Binding and Mechanism of Action of Novel Aspartate Aminotransferase Inhibitors. Biochemistry. 2018 Nov 27;57(47):6604-6614.
溶解度数据
In Vitro: DMSO : 100 mg/mL (312.12 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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