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] | |
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. |
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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 property | T1/2(h) | Tmax(h) | Cmax(ng/mL) | bioavailability F (%) | | i.v./i.p. | 2.31/0.77 | 0.25 | 5543.99/3878 | 52.55 |
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| 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. |
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