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。

IDO2-IN-1 is an orally active and potent Indoleamine 2,3-dioxygenase 2 (IDO2) inhibitor with an IC 50 value of 112 nM. IDO2-IN-1 can be used for inflammatory autoimmunity research.

Solid

IDO1 411 nM (IC50) IDO2 112 (IC50

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.
has not independently confirmed the accuracy of these methods. They are for reference only.Cell Viability Assay

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

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

[1]. He G, et al. Discovery of the First Selective IDO2 Inhibitor As Novel Immunotherapeutic Avenues for Rheumatoid Arthritis. J Med Chem. 2022 Aug 11.

In Vitro: DMSO : 140 mg/mL (258.61 mM; Need ultrasonic)配制储备液