产品
编 号：F758351
分子式：C14H10N4
分子量：234.26
分子式：C14H10N4
分子量：234.26
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
50mg
询价
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100mg
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结构图
CAS No: 461424-21-5
产品详情
生物活性：
IDO1/TDO-IN-4 is a potent IDO1/TDO dual inhibitor, with IC50 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 disorders.
体内研究：
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.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.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 T1/2 (h)Tmax (h) Cmax (ng/mL)bioavailability F (%)
i.v./i.p. 2.31/0.770.25 5543.99/387852.55
体外研究：
IDO1/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.
IDO1/TDO-IN-4 is a potent IDO1/TDO dual inhibitor, with IC50 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 disorders.
体内研究：
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.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.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 T1/2 (h)Tmax (h) Cmax (ng/mL)bioavailability F (%)
i.v./i.p. 2.31/0.770.25 5543.99/387852.55
体外研究：
IDO1/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.
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