IDO1/TDO-IN-4 (C09-1140-099)

IDO1/TDO-IN-4 is a potent IDO1/TDO dual inhibitor, with IC 50 values of 3.53 μM (IDO1) and 1.15 μM (TDO). IDO1/TDO-IN-4 forms hydrogen bond with IDO1 , 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 disordersIn VitroIDO1/TDO-IN-4 (compound 28, 0-2 μM, 1 h) inhibits the LPS-induced activation of BV2 microglial cells (determined by morphological changes). IDO1/TDO-IN-4 (0-2 μM, 1 h) inhibits the generation of pro-inflammatory factors and promotes the expression of IL-10. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. RT-PCRCell 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.In VivoIDO1/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 . 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 2 mg/kg LPS-induced depressive mice 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) 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 52.55Form:SolidIC50& Target:IDO1 3.53 μM (IC 50 ). Specification: 0.99 Molecular Formula: C14H10N4 Molecular Weight: 234.26