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IDO1/TDO-IN-4
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。
IDO1/TDO-IN-4图片
CAS NO:461424-21-5
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
IDO1/TDO-IN-4 是一种有效的IDO1/TDO双重抑制剂,IC50值为 3.53 μM (IDO1) 和 1.15 μM (TDO)。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、以及抑郁引起的感染性疾病、代谢性疾病和自身免疫性疾病的研究。
生物活性

IDO1/TDO-IN-4 is a potentIDO1/TDOdual inhibitor, withIC50values of 3.53 μM (IDO1) and 1.15 μM (TDO). IDO1/TDO-IN-4 forms hydrogen bond withIDO1, and π–π stacking interaction with TDO. IDO1/TDO-IN-4 can be used in the research of depression, and depression-induced infectious, metabolic, and autoimmune disorders[1].

IC50& Target[1]

IDO1

3.53 μM (IC50)

体外研究
(In Vitro)

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) decreases the expression of IDO1 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.
体内研究
(In Vivo)

IDO1/TDO-IN-4 (compound 28, i.p., 20 mg/kg, at day 1, 2, 3) rescues LPS-induced neuroinflammation and depressive-like behavior in mice[1].
IDO1/TDO-IN-4 (I.p. or i.v., 20 mg/kg) displays 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 propertyT1/2(h)Tmax(h)Cmax(ng/mL)bioavailability F (%)
i.v./i.p.2.31/0.770.255543.99/387852.55
分子量

234.26

Formula

C14H10N4

CAS 号

461424-21-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.