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MedChemExpress - Model IDO2-IN-1 - ...

MedChemExpress - Model IDO2-IN-1 - 2803768-09-2

IDO2-IN-1 is an orally active and potent Indoleamine 2,3-dioxygenase 2 (IDO2) inhibitor with an IC50 value of 112 nM. IDO2-IN-1 can be used for inflammatory autoimmunity research[1].

IDO2-IN-1

MCE China：IDO2-IN-1

Brand：MedChemExpress (MCE)

Cat. No.HY-151093

CAS：2803768-09-2

Purity：98.86%

Storage：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)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：IDO2-IN-1 is an orally active and potent Indoleamine 2,3-dioxygenase 2 (IDO2) inhibitor with an IC50 value of 112 nM. IDO2-IN-1 can be used for inflammatory autoimmunity research.

In Vitro：IDO2-IN-1 (compound 22) shows stronger inhibition on IDO2 (IC50 =112 nM) over IDO1 (IC50 =411 nM)[1]. 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[1].

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[1]. 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[1]. 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[1]. Pharmacokinetic Profile in Rat[1] Route Dose (mg/kg) T1/2/sub> (h) Tmax (h) Cmax (ng/mL) AUC(0-∞) (h•ng/mL) CL (mL/h/kg) Vz (mL/kg) MRT(0-∞) (h) F (%) i.v. 1 0.69 / / 375.1 2673 2675 0.55 / p.o. 10 2.02 0.75 153.8 670.5 / / 7.48 17.87

IC50 & Target：IDO1 411 nM (IC50) IDO2 112 (IC50)

References：

[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. [Content Brief]

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