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IDO2-IN-1

CAS No. :

MCE 站：IDO2-IN-1

产品活性：IDO2-IN-1 是一种具有口服活性的强效吲哚胺 2,3- 双加氧酶 (IDO2) 抑制剂，IC₅₀ 为 112 nM。IDO2-IN-1 能够用于对炎症性自身免疫的研究。

研究领域：Metabolic Enzyme/Protease

作用靶点：Indoleamine 2,3-Dioxygenase (IDO)

In Vitro: IDO2-IN-1 (compound 22) shows stronger inhibition on IDO2 (IC₅₀ =112 nM) over IDO1 (IC₅₀ =411 nM).
IDO2-IN-1 inhibits hIDO1 expression (EC₅₀=633 nM) in HeLa cell-based IDO1/kynurenine assay, co-incubated with hIFN-γ (100 ng/mL final concentration), which is used for producing N-formylkynurenine.

In Vivo: The Adjuvant arthritis (AA) model ａnd Collagen-induced arthritis (CIA) model have similar pathogenesis ａnd pathological characteristics to human rheumatoid arthritis (RA).
IDO2-IN-1 (compound 22) (100 mg/kg; p.o.; once dose) exhibits excellent anti-inflammatory activity, higher than naproxen, a prescription drug reducing pain, swelling, ａnd joint stiffness from arthritis.
IDO2-IN-1 (25, 50, 100 mg/kg; i.p.; once daily, for 19 d) exhibits excellent inhibitory effect on mice paw swelling, shows efficacy in a collagen-induced arthritis model in mice.
IDO2-IN-1 (30, 60, 120 mg/kg; i.p.; once daily, for 15 d) inhibits joint inflammation ａnd displays potential effect in autoimmune arthritis improvement.
Pharmacokinetic Profile in Rat

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