Powder: -20°C for 3 years | In solvent: -80°C for 1 year
IDO1/TDO-IN-4 显示出对 IDO1 (IC50 = 3.53 μM) 和 TDO (IC50 = 1.15 μM) 的有效抑制作用,并且具有可接受的安全性和药代动力学特性。IDO1/TDO-IN-4 可与 IDO1 形成氢键,与 TDO 产生 π-π 堆积相互作用。 IDO1/TDO-IN-4 可用于抑郁症以及炎症引起的抑郁症的研究。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 652 | 5日内发货 | ||
5 mg | ¥ 1,080 | 5日内发货 | ||
10 mg | ¥ 1,950 | 5日内发货 |
产品描述 | IDO1/TDO-IN-4 displays potent inhibition of both IDO1 (IC50 = 3.53 μM) and TDO (IC50 = 1.15 μM) and has an acceptable safety profile and pharmacokinetic properties. IDO1/TDO-IN-4 forms a hydrogen bond with IDO1, and π π stacking interaction with TDO. IDO1/TDO-IN-4 can be used in the research of depression and inflammation-induced depression [1]. |
体外活性 | IDO1/TDO-IN-4 (compound 28, 0-2 μM, 1 h) inhibits the LPS-induced activation of BV2 microglial cells (determined by morphological changes) [1]. IDO1/TDO-IN-4 (0-2 μM, 1 h) inhibits the generation of pro-inflammatory factors and promotes the expression of IL-10 [1]. IDO1/TDO-IN-4 (0-2 μM, 1 h) reduces the IDO1 expression and prevents the excessive degradation of tryptophan via the kynurenine pathway [1]. RT-PCR [1] Cell Line: 100 ng/mL LPS-induced BV2 microglial cells Concentration: 0, 0.25, 0.5, 1, 2 μM Incubation Time: 1 h Result: Inhibited the generation of COX2, iNOS, TNF-α, and IL-1β. Increased the level of IL-10. |
体内活性 | IDO1/TDO-IN-4 (compound 28, i.p., 20 mg/kg, at day 1, 2, 3) attenuates LPS-induced neuroinflammation and depressive-like behavior in mice [1]. IDO1/TDO-IN-4 (I.p. or i.v., 20 mg/kg) exhibits high exposure and a high volume of distribution at the steady state in normal mice [1]. Animal Model: 2 mg/kg LPS-induced depressive mice [1] Dosage: 20 mg/kg Administration: Intraperitoneal injection (i.p.), at day 1, 2, 3. Result: Attenuated microglial activation significantly. Decreased inflammatory factors in the hippocampus, such as TNF-α, IL-1β, and iNOS. Downregulated LPS-induced overexpression of IDO1. Animal Model: Male C57BL/6J mice (pharmacokinetic assay) [1] Dosage: 20 mg/kg Administration: Intraperitoneal injection and intravenous injection Result: Pharmacokinetic profile of IDO1/TDO-IN-4 (compound 28) pharmacokinetic property T 1/2 (h) T max (h) C max (ng/mL) bioavailability F (%) i.v./i.p. 2.31/0.77 0.25 5543.99/3878 52.55 |
分子量 | 234.26 |
分子式 | C14H10N4 |
CAS No. | 461424-21-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
IDO1/TDO-IN-4 461424-21-5 Inhibitor inhibitor inhibit